Search

Purpose To correlate the apparent diffusion coefficient (ADC) of endometrioid carcinoma with histological tumor grade and degree of myometrial invasion. Materials and Methods 3T diffusion-weighted (DW) magnetic resonance (MR) images of 63 patients were retrospectively reviewed. Two readers measured tumor ADC according to a freehand region of interest (ROI) and a round ROI. Mean and minimum ADCs were correlated with prognostic parameters. Results The minimum ADC was 0.64 × 10−3mm2/s for grade 1 (G1, n = 42), 0.62 for grade 2 (G2, n = 14), 0.46 for grade 3 (G3, n = 7) on freehand ROI. There were significant differences between G1 and G3 (P = 0.007), and G2 and G3 (P = 0.038). No significant correlation was found between tumor grade and mean ADC (0.85 for G1, 0.82 for G2, and 0.72 for G3, P = 0.166). The minimum ADC was significantly lower for patients with deep (n = 21, 0.54) than for those with superficial (n = 39, 0.65) myometrial invasion. Conversely, mean ADC did not differ significantly (0.84 for superficial and 0.78 for deep myometrial invasion, P = 0.081). The same tendency was shown on round ROI. Conclusion The minimum ADC correlates with prognostic parameters of endometrial carcinoma more strongly than mean ADC. Lower minimum ADC is associated with higher histological tumor grade and higher degree of myometrial invasion. J. Magn. Reson. Imaging 2015;41:213–219. © 2013 Wiley Periodicals, Inc.

Purpose To investigate the influence of different-shaped regions of interest (ROIs) on tumor apparent diffusion coefficient (ADC) measurements and interobserver variability in endometrial carcinoma. Materials and Methods Sixty-nine patients (age range, 32–92 years; mean, 61 years) were evaluated in this retrospective study. Patients had undergone magnetic resonance (MR) examinations including diffusion-weighted imaging (DWI) using a 3.0-T MR system. Two readers measured tumor ADCs using four ROI methods: freehand ROI; square ROI; round ROI; and five small, round ROIs. Minimum and mean ADCs were obtained. The interclass correlation coefficient (ICC) was statistically analyzed to assess measurement reliability. Repeated-measures analysis of variance was used for comparisons of ADCs measured with each ROI method. Results ICCs were 0.93 (minimum ADC) / 0.93 (mean ADC) for freehand ROIs, 0.94/0.95 for square ROIs, 0.94/0.95 for round ROIs, and 0.95/0.96 for five small, round ROIs. All ROI methods indicated excellent correlations. Each minimum ADC was significantly different except between square ROI and round ROI (P < 0.001). Mean ADCs showed significant differences only between freehand ROI and the other ROI methods (P < 0.001). Conclusion ROI shape has no marked influence on ICC in endometrial carcinoma. Compared with minimum ADCs, mean ADCs are suggested to provide more stable results regardless of the ROI method. J. Magn. Reson. Imaging 2014;40:157–161. © 2013 Wiley Periodicals, Inc.

a counterion for the isolation of reactive cations, and for activation of catalysts in organic synthesis. Its unique electronic and molecular structures render 1 as an attractive starting material for the construction of various functional molecules and bioactive/pharmaceutical building blocks. However, progress in the synthesis of such materials is hindered by the lack of methods for the functionalization of 1. In particular, no efficient general methods are available for introduction of aryl and sp/sp-hybridized carbon centers at the carbon vertex of C1-carborane. A cross-coupling reaction is an obvious method for the introduction of aryl groups and sp/sp-hybridized carbon centers at the carbon vertex of C1-carborane derivatives, but has not yet been successful. 10] The intrinsic difficulty appears to be associated mainly with the sterically hindered and hypervalent nature of the vertex carbon atom in 1. We report herein a general and efficient copper-mediated C C cross-coupling reaction of 1 under palladium catalysis that yields a variety of C-functionalized C1-carborane derivatives and provides a basic architecture for pharmacophores and functional materials. The reaction is demonstrated not only for the parent C1-carborane but also its B-halogenated derivatives. To demonstrate utility of the method and the resulting new class of compounds, we describe the synthesis of multivalent anions and disclose preliminary results of the biological activity and liquid crystal behavior of selected derivatives. We commenced our studies by screening for a suitable metal species at the C1-carborane carbon vertex for crosscoupling reaction with aryl iodide 2a under palladium catalysis (Table 1). Reactions of various zinc carborate derivatives 1a (i.e. Negishi-type reaction), including zincate complexes, were unsuccessful (Table 1, entry 1). The Suzuki–Miyaura-type cross-coupling with pinacol borate 1b was also examined under a variety of conditions, but failed to give the desired product, affording only halogenated C1carboranes, with most of the pinacol borate moiety remaining intact (Table 1, entry 2). These results imply that the nature of the vertex carbon atom with respect to transmetalation is quite different from that of typical aryl or alkyl carbon atoms. After extensive screening of other systems, we found that a combination of copper(I) carborate 1c and a palladium catalyst promoted the coupling reaction with 2a at room temperature to give the desired product 3a (Table 1, Scheme 1. C1-carborane (1).

BACKGROUND AND PURPOSE: Progressive changes in the substantia nigra pars compacta and locus ceruleus of patients with Parkinson disease and Alzheimer disease visualized by neuromelanin MRI and cardiac postganglionic sympathetic nerve function on (123)I-metaiodobenzylguanidine scintigraphy have not been fully evaluated. We compared the diagnostic value of these modalities among patients with early Parkinson disease, late Parkinson disease, and Alzheimer disease. MATERIALS AND METHODS: We compared contrast ratios of signal intensity in medial and lateral regions of the substantia nigra pars compacta and locus ceruleus with those of the tegmentum of the midbrain and the pons, respectively, by use of neuromelanin MRI in patients with early Parkinson disease (n = 13), late Parkinson disease (n = 31), Alzheimer disease (n = 6), and age-matched healthy control subjects (n = 20). We calculated heart-to-mediastinum ratios on (123)I-metaiodobenzylguanidine scintigrams after setting regions of interest on the left cardiac ventricle and upper mediastinum. RESULTS: The signal intensity of the lateral substantia nigra pars compacta on neuromelanin MRI was significantly reduced in early and late Parkinson disease, and that of the medial substantia nigra pars compacta was gradually and stage-dependently reduced in Parkinson disease. The signal intensity of the locus ceruleus was obviously reduced in late Parkinson disease. Signal reduction was not significant in the substantia nigra pars compacta and locus ceruleus of patients with Alzheimer disease. The heart-to-mediastinum ratio on (123)I-metaiodobenzylguanidine scintigrams was stage-dependently reduced in Parkinson disease and normal in Alzheimer disease. The signal intensity ratios in substantia nigra pars compacta and locus ceruleus on neuromelanin MRI positively correlated with the heart-to-mediastinum ratio on (123)I-metaiodobenzylguanidine scintigrams. CONCLUSIONS: Both neuromelanin MRI and (123)I-metaiodobenzylguanidine scintigraphy can help to evaluate disease progression in Parkinson disease and are useful for differentiating Parkinson disease from Alzheimer disease.

BACKGROUND AND PURPOSE: The risk of hemorrhage in the context of developmental venous anomaly is considered to be very low, but it has never been evaluated by susceptibility-weighted MR imaging at 3T. The goal of the present study was to evaluate the prevalence of hypointense foci (ie, microhemorrhage or cavernous malformation) associated with DVA on phase-sensitive MR imaging, on the basis of principles similar to those of susceptibility-weighted MR imaging, and to evaluate the relationship between the hypointense foci and several factors, such as white matter hyperintense lesions adjacent to DVA on T2-weighted imaging, DVA morphology, and clinical symptoms. MATERIALS AND METHODS: This study retrospectively evaluated 61 lesions in 59 consecutive patients with DVA who underwent MR imaging including phase-sensitive MR imaging. Two neuroradiologists independently assessed for the presence of hypointense foci and other factors such as DVA location, depth, size, direction of draining vein on phase-sensitive MR imaging, and white matter hyperintense lesion on T2-weighted imaging. Clinical symptoms were also assessed. RESULTS: Hypointense foci were observed in 62.3% (38/61) of lesions. White matter hyperintense lesion was more frequently observed in patients with hypointense foci (26/38) than in patients without hypointense foci (7/23) (P < .01). There was no significant association between hypointense foci and other factors. CONCLUSIONS: Our results support the hypothesis that microhemorrhage or cavernous malformation can be related to venous congestion caused by abnormal venous drainage. We conclude that phase-sensitive MR imagingis useful for the detection of microhemorrhage or cavernous malformation in patients with DVA, especially when associated with white matter hyperintense lesion.

Objective: We investigated the appropriate reconstruction interval required to generate optimal quality images of the coronary veins and to evaluate the size of each vein at the systolic and diastolic phases using coronary computed tomography (CT) venography. Methods: Coronary CT venograms obtained from 30 patients using 64-slice CT were reconstructed at 0% to 90% of the cardiac cycle in 10% increments. Two radiologists assessed the image quality of the anterior interventricular vein (AIV), the great cardiac vein (GCV), the posterior vein of the left ventricle (PVLV), the posterior interventricular vein (PIV), the coronary sinus (CS) and the small cardiac vein (SCV). We determined the sizes of measurable CS (n = 16) and GCV (n = 12) at the end systolic and mid diastolic phases. Results: The most appropriate reconstruction point for all coronary veins turned out to be at the mid-diastolic phase. The size of the CS and GCV was greater at a 30% than that at a 70% R-R interval (p Conclusions: Image quality was optimal at the mid-diastolic phase for each coronary vein, but the sizes of the coronary veins varied during the cardiac cycle. The cardiac cycle must be considered when measuring the sizes of cardiac veins.

Purpose: The characteristics of fetal thyroid on magnetic resonance (MR) imaging, including normal thyroid and disorders other than goiter have not been fully evaluated. Our aim was to assess fetal thyroid using three dimensional (3D) gradient echo (GRE) T1-weighted MR imaging and to examine the usefulness of this modality. Materials and Methods: The study included 27 3D GRE T1-weighted images from 26 fetuses. The largest possible region of interest (ROI) within the thyroid at the slice level depicting the thyroid was manually defined and three circular ROIs on neck muscle were manually defined on the image slices showing the highest signal intensity (SI) of the thyroid. Maximum and mean thyroid-to-muscle SI ratios (SIRs) were then calculated as SIR = maximum or mean thyroid SI/muscle SI. Results: The thyroid could not be identified in two cases. Fetal thyroid function was normal in 17 cases, and there were 7 cases of hypothyroidism (6 transient and 1 thyroid dysgenesis). There was no linear relationship between mean and maximum SIR and gestational age. The mean and maximum SIR in the cases of normal fetal thyroid were 1.85 ± 0.20 and 2.61 ± 0.39, and the mean and maximum SIR in fetal hypothyroidism were 1.58 ± 0.20 and 2.13 ± 0.37. Mean (P = 0.0088) and maximum (P = 0.0221) SIR values were significantly different between euthyroid and hypothyroid fetuses. Conclusion: Thyroid SIR measurement provided useful information regarding fetal thyroid function.

Anti-inflammatory pharmacotherapy for asthma has mainly depended on the inhalation of glucocorticoids, which non-specifically suppress immune responses. If the anti-inflammatory cytokine interleukin (IL)-10 can be induced by a specific antigen, asthmatic airway inflammation could be suppressed when individuals are exposed to the antigen. The purpose of this study was to develop cellular immunotherapeutics for atopic diseases using IL-10-producing CD4

Progesterone is involved in multiple physiological processes, including female reproduction, via binding to the progesterone receptor (PR). We have developed 6-arylcoumarins such as 5 and 6 as non-steroidal PR antagonists with receptor-binding-dependent fluorescence. In this study, we investigated the structure–activity relationships and fluorescence properties of coumarin derivatives bearing a heterocyclic aromatic moiety. Among these derivatives, 7c (IC50: 34 nM) and 10b (IC50: 24 nM) showed more potent PR-antagonistic activity than lead compounds 5 (IC50: 500 nM) and 6 (IC50: 65 nM) in alkaline phosphatase (AP) assay. Compound 9b showed solvent-dependent fluorescence intensity, exhibiting strong fluorescence in the presence of PR LBD only in buffer solution. On the other hand, 10b showed a solvent-dependent shift of the fluorescence maximum wavelength in the presence of PR LBD. These results indicate that 6-arylcoumarin will be a useful scaffold for PR antagonists and fluorescent probes targeting PR.

Graves' ophthalmopathy (GO) is a common manifestation of Graves' disease (GD); however, its pathogenesis is not well understood. Recently, the dysregulation of regulatory T cells (Tregs) has been thought to be closely associated with the pathogenesis and clinical symptoms of autoimmune disease. We therefore evaluated whether T cell subsets, including Tregs, are associated with GO pathogenesis and clinical symptoms. In this observational study we evaluated 35 GD patients with overt ophthalmopathy (GOs) and 28 patients without ophthalmopathy (non-GOs). Fifteen healthy euthyroid patients served as healthy controls (HCs). Peripheral blood mononuclear cells from GOs, non-GOs and HCs were analyzed for CD4, CD25, and FoxP3 expression using flow cytometry. We also evaluated their correlation with disease activity according to the clinical activity score (CAS) and magnetic resonance imaging (MRI) findings. Disease severity was evaluated using the NOSPECS score, and clinical progression of GO was followed for 24 weeks. The main outcome measures were the frequencies of FoxP3-positive and -negative CD4(+) CD25(+) T cells at study outset, namely Tregs and effector T cells (Teffs), respectively. GOs had higher frequencies of Teffs (30.8±8.4%) than non-GOs (19.4±7.1%) and HCs (22.7±7.9%). Notably, patients with improved GOs had lower frequencies of Tregs (5.8±1.1%) than patients with stable or deteriorated GOs (7.3±1.2%), although ophthalmic and radiological parameters were not significantly different at the start of the study. In conclusion, an expanded Teff population may be associated with GO pathogenesis. Additionally, decreased Tregs in peripheral blood may predict a good clinical outcome.

Motor learning is a process whereby the acquisition of new skills occurs with practice, and can be influenced by the provision of feedback. An important question is what frequency of feedback facilitates motor learning. The guidance hypothesis assumes that the provision of less augmented feedback is better than more because a learner can use his/her own inherent feedback. However, it is unclear whether this hypothesis holds true for all types of augmented feedback, including for example sonified information about performance. Thus, we aimed to test what frequency of augmented sonified feedback facilitates the motor learning of a novel joint coordination pattern. Twenty healthy volunteers first reached to a target with their arm (baseline phase). We manipulated this baseline kinematic data for each individual to create a novel target joint coordination pattern. Participants then practiced to learn the novel target joint coordination pattern, receiving either feedback on every trial i.e., 100% feedback (n = 10), or every other trial, i.e., 50% feedback (n = 10; acquisition phase). We created a sonification system to provide the feedback. This feedback was a pure tone that varied in intensity in proportion to the error of the performed joint coordination relative to the target pattern. Thus, the auditory feedback contained information about performance in real-time (i.e., "concurrent, knowledge of performance feedback"). Participants performed the novel joint coordination pattern with no-feedback immediately after the acquisition phase (immediate retention phase), and on the next day (delayed retention phase). The root-mean squared error (RMSE) and variable error (VE) of joint coordination were significantly reduced during the acquisition phase in both 100 and 50% feedback groups. There was no significant difference in VE between the groups at immediate and delayed retention phases. However, at both these retention phases, the 100% feedback group showed significantly smaller RMSE than the 50% group. Thus, contrary to the guidance hypothesis, our findings suggest that the provision of more, concurrent knowledge of performance auditory feedback during the acquisition of a novel joint coordination pattern, may result in better skill retention.

The coordination of body movements to a musical beat is a common feature of many dance styles. However, the auditory-motor coordination skills of dancers remain largely uninvestigated. The purpose of this study was to examine the auditory-motor coordination skills of non-dancers, street dancers, and the winner of a celebrated international street dance competition, while coordinating their rhythmic finger movements to a beat. The beat rate of a metronome increased from 1.0 to 3.7 Hz. The participants were asked to either flex or extend their index fingers on the beat in each condition. Under the extend-on-the-beat condition, both the dancers and non-dancers showed a spontaneous transition from the extend-on-the-beat to the flex-on-the-beat or to a phase wandering pattern. However, the critical frequency at which the transition occurred was significantly higher in the dancers (3.3 Hz) than in the non-dancers (2.6 Hz). Under the flex-on-the-beat condition, the dancers were able to maintain their coordination pattern more stably at high beat rates compared to the non-dancers. Furthermore, the world champion matched the timing of movement peak velocity to the beat across the different beat rates. This may give a sense of unity between the movement and the beat for the audience because the peak velocity of the rhythmic movement works as a temporal cue for the audiovisual synchrony perception. These results suggest that the skills of accomplished dancers lie in their small finger movements and that the sensorimotor learning of street dance is characterized by a stabilization of the coordination patterns, including the inhibition of an unintentional transition to other coordination patterns.

1From the Department of Abdominal Imaging, St Eloi University Hospital, CHU Montpellier, 80 Avenue Augustin Fliche, Montpellier, 34295 France (S.N., E.D., B.G.); Department of Radiology, Memorial Sloan Kettering Cancer Center, New York, NY (Y.L., E.S.); Department of Radiology, McGill University Health Centre, Montreal, QC, Canada (C.R.); Department of Radiology, Addenbrooke’s Hospital, Cambridge, England (H.C.A.); Division of Radiology, Department of Pathophysiological and Therapeutic Science, Faculty of Medicine, Tottori University, Yonago, Japan (S.F.); IRCM, Institut de Recherche en Cancerologie de Montpellier, Montpellier, France (S.N., B.G.); and INSERM, Unit 896, Montpellier, France (S.N., B.G.). Received June 15, 2015; revision requested October 6 and received November 1; accepted November 14. All authors have disclosed no relevant relationships. Address correspondence to S.N. (email: stephanienougaret@free.fr).

We report the design, synthesis, and physicochemical/biological evaluation of novel silanol derivative 6 (sila-T) as a silanol analog of multi-target nuclear receptor modulator T0901317 (5). Compound 6 showed intermediate hydrophobicity between the corresponding alcohol 13 and perfluoroalcohol 5. While 5 exhibited potent activities toward liver X receptor α and β, farnesoid X receptor, pregnane X receptor (PXR) and retinoic acid receptor-related orphan receptor (ROR)γ, silanol 6 exhibited activity only toward PXR and RORs. Incorporation of silanol instead of perfluoroalcohol is a promising option for developing novel target-selective, biologically active compounds.

Purpose: To evaluate rectal cancer volumetry in predicting initial neoadjuvant chemotherapy response. Materials and Methods: Sixteen consecutive patients who underwent neoadjuvant chemotherapy (CX) before chemoradiotherapy (CRT) and surgery were enrolled in this retrospective study. Tumor volume was evaluated at the first magnetic resonance imaging (MRI), after CX and after CRT. Tumor volume regression (TVR) and downstaging were compared with histological results according to Tumor Regression Grade (TRG) to assess CX and CRT response, respectively. Results: The mean tumor volume was 132 cm3 ± 166 before and 56 cm3 ± 71 after CX. TVR after CX was significantly different between patients with poor histologic response (TRG1/2) and those with good histologic response (TRG3/4) (P = 0.001). An optimal cutoff of TVR >68% (area under the curve [AUC]: 0.9, 95% confidence interval [CI]: 0.65–0.98, P = 0.0001) to predict good histology response after CX was assessed by receiver operating characteristic curve. According to previous data and this study, we defined 70% as the best cutoff values according to sensitivity (86%), specificity (100%) of TVR for predicting good histology response. In contradistinction, MRI downstaging was associated with TRG only after CRT (P = 0.04). Conclusion: Our pilot study showed that MRI volumetry can predict early histological response after CX and before CRT. MRI volumetry could help the clinician to distinguish early responders in order to aid appropriate individually tailored therapies. J. Magn. Reson. Imaging 2013;38:726–732. © 2012 Wiley Periodicals, Inc.

Ovarian carcinoma is the most common cause of death due to gynecologic malignancy. Peritoneal involvement is present in approximately 70% of patients at the time of initial diagnosis. The disease spreads abdominally by direct extension, exfoliation of tumor cells into the peritoneal space, and dissemination of tumor cells along lymphatic pathways. Carcinomatosis characterizes an advanced stage of disease in which peritoneal disease has spread throughout the upper abdomen (stage IIIC) or in which diffuse peritoneal disease is accompanied by malignant pleural infiltration or visceral metastases (stage IV). Common sites of intraperitoneal seeding of ovarian carcinoma include the pelvis, omentum, paracolic gutters, liver capsule, and diaphragm. Soft-tissue thickening, nodularity, and enhancement are all signs of peritoneal involvement. Advanced-stage disease is treated either with initial cytoreductive surgery (debulking) followed by adjuvant chemotherapy, or with initial neoadjuvant chemotherapy followed by debulking. Radiologic imaging plays an important role in the selection of patients who may benefit from neoadjuvant chemotherapy before debulking. However, accurate interpretation of the imaging findings is challenging and requires a detailed knowledge of the complex peritoneal anatomy, directionality of flow of peritoneal fluid, and specific disease sites that are likely to present particular difficulties with regard to surgical access and technique. Although there is as yet no clear consensus on the criteria for resectability of peritoneal lesions, extensive involvement of the small bowel or mesenteric root, involved lymph nodes superior to the celiac axis, pleural infiltration, pelvic sidewall invasion, bladder trigone involvement, and hepatic parenchymal metastases or implants near the right hepatic vein are considered indicative of potential nonresectability. Implants larger than 2 cm in diameter in the diaphragm, lesser sac, porta hepatis, intersegmental fissure, gallbladder fossa, or gastrosplenic or gastrohepatic ligament also may represent nonresectable disease.

Spike shape analysis (SSA) is a method to infer motor unit (MU) activity by examining interference pattern of surface electromyography (sEMG). SSA has succeeded to assess neuromuscular adaptations after dynamic training; however, it has not been used to assess muscle activities during the dynamic movements as seen in music performance. The present study used SSA to investigate sEMG activities of wrist flexor and extensor muscles in the winner of a contest to find the world's fastest drummer (WFD) during performing rhythmic wrist flexion/extension movements with one hand using a handheld drumstick. SSA measures of the WFD were compared with those in the two control groups: non-drummers (NDs) and ordinary drummers (ODs). We found that the WFD showed significantly high mean spike frequency (MSF), short mean spike duration (MSD), and small mean number of peaks per spike (MNPPS) compared with the control groups. These results suggest that the WFD had exceptional MU activity such as higher MU discharge rate, more MU recruitment, and/or higher MU synchronization to achieve extraordinary fast 10-Hz drumming performance. SSA will be useful to investigate the muscle activity seen in music performance.

While novices who are unfamiliar to a new motor skill typically show variable and unstable movements, highly skilled experts show a stable and accurate performance. These distinct differences in motor control between experts and novices have led researchers to hypothesize that neuromotor noise is reduced in the process of motor skill acquisition. On the other hand, it should be noted that novices’ movements have other characteristics; they are habituated and stereotyped. In this review, we discuss the principles governing spatiotemporal organization of movements in novices and experts while solving specific motor problems under varied conditions, by introducing experimental and theoretical studies that use neurophysiological techniques such as electromyography, functional magnetic resonance imaging, and transcranial magnetic stimulation, and mathematical models such as stochastic and dynamical models. On the basis of the findings from a variety of perceptual-motor skills (e.g., ballthrowing, badminton smash, long-distance running, piano and drum performance, street dance, a popular hand game of rock-paper-scissors, and temporal order judgement task), we argue that the novices’ characteristic movement patterns were organized under specific constraints and typical strategy, without which the variability would increase even more, while experts’ movements were organized with functional and compensatory variability that can drive out erroneous noise variability. We also showed that in a particular type of interlimb coordination, skilled and unskilled movement patterns could be seamlessly described as the time evolution of nonlinear and self-organized dynamical systems, suggesting that the dynamical systems approach is a major candidate for understanding the principle underlying organization of experts’ and novices’ movements.

Various 6-arylcoumarin derivatives were designed and synthesized as candidate nonsteroidal type progesterone antagonists. 6-Bromocoumarin derivatives were prepared from the corresponding 4-substituted 2-acetoxy-5-bromobenzaldehyde by employing the Still-Gennari modification of the Horner-Wadsworth-Emmons olefination reaction and were converted to 6-arylcoumarins by means of Suzuki-Miyaura cross-coupling reactions. The biological activities of these coumarin derivatives were evaluated by means of alkaline phosphatase assay in the T47D human breast carcinoma cell line. Among the synthesized compounds, 36 (IC(50) = 0.12 μM) and 38 (IC(50) = 0.065 μM), bearing a five-membered heterocycle, showed potent PR antagonist activity. Competitive binding assay showed that compounds 8 and 34 have potent PR binding affinity. The fluorescence of compound 8 was dependent on the solvent properties and was increased in the presence of PR ligand binding domain. This property might be applicable to the development of fluorescence probes for studies on PR.

Riccardin C (RC, 1) is a macrocyclic bis(bibenzyl) natural product exhibiting remarkable biological activity as a nuclear liver X receptors (LXRs) ligand and a lipid metabolism mediator. RC is expected to be a lead compound to develop drugs for atherosclerotic diseases, and therefore exploiting diversity-oriented synthesis of RC is a promising approach to drug discovery. In this paper, we report novel total synthesis of RC (7.4% overall yield in 16 steps) by using the intramolecular SNAr reaction as key cyclization reaction. This is the first example of efficient macrocyclization using 3-nitro-4-fluorostilbene as an electrophile. The methodology could be applied to synthesize novel lactam analogs of RC. The diversity-oriented synthesis of RC is versatile method for the synthesis of various types of bis(bibenzyl) natural products and their derivatization.

the present study examined the synchronization error (SE) of drum kit playing by professional drummers with an auditory metronome, focusing on the effects of motor effectors and tempi. Fifteen professional drummers attempted to synchronize a basic drumming pattern with a metronome as precisely as possible at tempi of 60, 120, and 200 beats per minute (bpm). In the 60 and 120 bpm conditions, the right hand (high-hat cymbals) showed small mean SE (∼2 ms), whereas the left hand (snare drum) and right foot (bass drum) preceded the metronome by about 10 ms. In the 200 bpm condition, the right hand was delayed by about 10 ms relative to the metronome, whereas the left hand and right foot showed small SE (∼1 ms). The absolute values of SE were smaller than those reported in previous tapping studies. In addition, the time series of SE were significantly correlated across the motor effectors, suggesting that each limb synchronized in relation to the other limbs rather than independently with the metronome.

Objectives To evaluate the usefulness of administration of superparamagnetic iron oxide (SPIO) and magnetic resonance (MR) imaging for assessing the efficacy of radiofrequency (RF) liver ablation. Material and methods Using a protocol approved by the animal research committee of our university, nine RF liver ablations were performed in three miniature pigs. Six ablations were performed after administration of SPIO in two pigs (group A). Three ablations were performed in the other pig without administration of SPIO (group B). All pigs were sacrificed 4 days after the procedure. Harvested livers were scanned with a 1.5 T MR system before and after fixation with 10% buffered formalin, and MR images were precisely compared with histological specimens. Results There were no histological differences between the two groups. All ablated liver lesions showed coagulation necrosis at the external layer. There were no viable cells inside the coagulation necrosis. All ablated lesions had a hypointense rim on fast low angle shot (FLASH) images. The rims of group A were thicker than those of group B. The rims of group B corresponded histologically to congestion and hemorrhagic necrosis area. The rims of the group A corresponded to hemorrhagic necrosis and coagulation necrosis areas. In group A, the hypointense rim reflected necrotic Kupffer cells that took up SPIO before RF liver ablation. Conclusion Administration of SPIO made it possible to precisely evaluate ablated liver parenchyma by hypointense rim on FLASH images. This method is helpful for the evaluation of safety margin after RF ablation for liver tumors.

The purpose of this study was to investigate the efficacy of 3.0T MR imaging in the assessment of depth of myometrial invasion by endometrial carcinoma. Fifty women with histopathologically confirmed endometrial carcinoma underwent preoperative MR imaging at 3.0T. MR imaging findings were compared with microscopic pathologic findings in all cases. On evaluation of MR images and histopathological findings, myometrial invasion was classified as absent (tumor confined to the endometrium), superficial (less than 50% of myometrial thickness), or deep (50% or more of myometrial thickness) by two radiologists. The sensitivity, specificity, and accuracy of the MR imaging in distinguishing no myometrial invasion from myometrial invasion were 95/95, 60/70, and 88/90%, respectively, and no and superficial myometrial invasion from deep myometrial invasion were 88/94, 97/94, and 94/92%, respectively. In evaluation of the depth of myometrial invasion by endometrial carcinoma, 3.0T MR imaging has a high diagnostic accuracy that is equivalent to that of previously reported 1.5T MR imaging.

To elucidate the radiation-induced damage to the microstructure of the parotid gland using high-resolution magnetic resonance imaging.High-resolution magnetic resonance imaging of the parotid gland was performed before radiotherapy (RT) and during the RT period oror =3 weeks after RT completion for 12 head-and-neck cancer patients using a 1.5-T scanner with a microscopy coil. The maximal cross-sectional area of the gland was evaluated, and changes in the internal architecture of the gland were assessed both visually and quantitatively.Magnetic resonance images were obtained at a median parotid gland dose of 36 Gy (range, 11-64). According to the quantitative analysis, the maximal cross-sectional area of the gland was reduced, the width of the main duct was narrowed, and the intensity ratio of the main duct lumen to background was significantly decreased after RT (p.0001). According to the visual assessment, the width of the main duct tended to narrow and the contrast of the duct lumen tended to be decreased, but no significant differences were noted. The visibility of the duct branches was unclear in 10 patients (p = .039), and the septum became dense in 11 patients (p = .006) after RT.High-resolution magnetic resonance imaging is a noninvasive method of evaluating radiation-induced changes to the internal architecture of the parotid gland. Morphologic changes in the irradiated parotid gland were demonstrated during the RT course even when a relatively small dose was delivered to the gland.

The aim of this study was to investigate the spatiotemporal characteristics of rhythmic, stationary basketball bouncing in skilled and unskilled adult basketball players. Skilled ( n = 12) and unskilled ( n = 11) basketball players were asked to bounce a basketball every 700 msec, in as temporally stable and spatially accurate a manner as possible, while keeping their eyes fixed straight ahead. Spatial analyses revealed a lower variability of the ball bouncing point and less deviation from a target point in the performance of skilled players compared to unskilled players. Temporal analyses revealed no significant difference in variability of the interbounce interval in skilled versus unskilled players. However, skilled players had longer and more consistent contact time between hand and ball compared to the unskilled players. These results suggest that longer and more consistent hand contact with the ball play an important role in spatial control of basketball bouncing position.

Ovarian stromal hyperthecosis is characterized by diffuse distribution of luteinized stromal cells accompanied by varying degrees of stromal hyperplasia. We report a case of ovarian stromal hyperthecosis with particular regard to magnetic resonance (MR)–pathologic correlation. At initial MR imaging, the central areas of the bilateral ovarian masses showed hypointensity on T1-weighted images and hyperintensity on T2-weighted images, while the peripheries of the bilateral masses showed isointensity to myometrium on T1-weighted images and heterogeneous signal intensities on T2-weighted images. At 15 days after the initial MR imaging examination, a second MR imaging demonstrated shrinkage of the bilateral ovarian masses. Change in the peripheries to predominantly isointensity to myometrium on the T2-weighted images was also observed. The patient underwent bilateral oophorectomy. Microscopic examination revealed scattered nests of lutein cells on a background of densely proliferated ovarian stroma with minimal collagen production in both ovaries. Edema was occasionally seen in the outer portion but was marked in the central zone of the ovaries, particularly on the left. The final pathologic diagnosis was stromal hyperthecosis. With regard to MR–pathologic correlation, the MR findings in the peripheries of the bilateral masses (isointensity relative to myometrium on both T1- and T2-weighted imaging) showed the characteristics of stromal hyperthecosis.

Studies of rapid unimanual tapping have assumed that the human rate limit for voluntary rhythmic movement is 5-7 Hz, which corresponds to an inter-tap interval (ITI) of 150-200ms. In fact, the winner of a recent contest to find the world's fastest drummer (WFD) can perform such movements using a handheld drumstick at 10 Hz, which corresponds to an ITI of 100 ms. Because the contest measured only the number of taps by the WFD, we examined the stability of the ITI and the underlying wrist muscle activity of the WFD. By comparing the performance and wrist muscle activity of the WFD with those of two control groups (non-drummers (NDs) and ordinary skilled drummers (ODs)), we found that the WFD had a relatively stable ITI and more pronounced reciprocal wrist muscle activity during the 10-Hz performance. Our result indicates that very fast, stable tapping performance can be achieved by keeping the wrist joint compliant rather than stiff.

The conformational change of amide structure of benzanilide or urea structure of N , N ′-diphenylurea induced by methylation of the secondary nitrogen was visualized by introduction of pyrene moieties on the benzene ring. In contrast to the extended trans-form of secondary amide and urea, which showed monomer fluorescence emission of pyrene, the corresponding N-methylated compounds exist in cis-form, which exhibited excimer emission.

Phase-sensitive imaging, based on principles similar to those of susceptibility-weighted imaging, has enabled noninvasive visualization of cerebral veins and shed light on the analysis of venous architecture. In this review, the cerebral venous anatomy on phase-sensitive imaging is shown. Phase-sensitive imaging can clearly demonstrate the basal cerebral vein and deep cerebral veins: the medial group of subependymal veins such as the septal, posterior septal, and medial atrial veins and the lateral group of the subependymal veins such as the thalamostriate, direct lateral, and inferior lateral veins. Phase-sensitive imaging is useful for the understanding of cerebral venous anatomy.

Purpose To clarify the diagnostic accuracy of diffusion-weighted imaging (DWI) in differentiating benign from malignant ovarian lesions. Materials and Methods We retrospectively analyzed magnetic resonance images of 123 ovarian lesions in 119 patients. We defined lesions with abnormal signal intensity as malignancy and assessed the location of abnormal intensity within the lesions on DWI. We also assessed the mean and lowest apparent diffusion coefficient (ADC) values of the solid portion for each ovarian lesion. Results The majority of malignant ovarian tumors and mature cystic teratomas, and almost half of the endometriomas, showed abnormal signal intensity on DWI, whereas most fibromas and other benign lesions did not. The main locations of abnormal signal intensity were solid portions in malignant ovarian tumors, cystic components suggestive of keratinoid substances and Rokitansky protuberance in mature cystic teratomas, and intracystic clots in endometriomas. On DW imaging, receiver-operating characteristic analysis yielded mean Az values of 0.703. There was no significant difference in mean and lowest ADC values between malignant and benign lesions. Conclusion DWI of ovarian lesions and ADC values of the solid component are not useful for differentiating benign from malignant ovarian lesions. This knowledge is essential in avoiding misinterpretation in the diagnosis of ovarian lesions. J. Magn. Reson. Imaging 2008;28:1149–1156. © 2008 Wiley-Liss, Inc.

We herein report a 12-year-old girl with a basal ganglia germinoma who presented with right-sided hemiparesis after a minor head trauma. Magnetic resonance (MR) imaging revealed a minimally enhanced lesion involving the left putamen, thalamus, and corona radiata. The lesion showed low-signal intensity on T1-, and high intensity on T2- and diffusion-weighted imaging. The MR signal in the adjacent globus pallidum was also low on T2-weighted imaging. MR spectroscopy on the lesion showed a large lactate/lipid/macromolecule peak with a decreased NAA/Cr ratio, but no increase in the Cho/Cr ratio. However, posttraumatic infarction at the territory of lateral lenticulostriate artery was ruled out 1 month later. This was based on progression of the hemiparesis and neuroimaging results, including an increased Cho/Cr ratio and weak uptake on (11)C-methionine positron emission tomography of the basal ganglia lesion. Stereotaxic brain biopsy confirmed the diagnosis of germinoma.

Posterior putaminal atrophy, putaminal T2-hyper and/or hyposignal changes have been observed in patients with multiple system atrophy (MSA) with parkinsonism.Postmortem T2-weighted images were compared with histological findings in seven autopsy-proven cases of putaminal lesions of MSA. All cases were evaluated on 1.5T magnetic resonance imaging (MRI) scanners and three cases were evaluated on 3T scanners.There were three types of putaminal changes: Type 1, mild putaminal atrophy and isointensity; Type 2, putaminal atrophy and diffuse hyperintensity with a hyperintense putaminal rim (HPR); Type 3, putaminal atrophy and iso-or-hypointensity with HPR. The signal intensities of the putamen in Types 1 and 3 were more hypointense on 3T images than on 1.5T images. In Type 1, mild putaminal atrophy showed mild neuronal loss and gliosis and diffuse ferritin deposition. In Types 2 and 3, the areas of putaminal atrophy, severe in the posterior region, showed severe neuronal loss and gliosis, many pigments that were positive for ferritin and Fe (3+) and diffuse ferritin deposition. Although, tissue rarefaction was more severe in Type 2 than in Type 3, pigment deposition was more severe in Type 3. The HPR showed a severe loss of myelin and axons with tissue rarefaction of the external capsule or putaminal rim in Types 2 and 3.Posterior putaminal atrophy reflects neuronal loss and gliosis. While putaminal iso-or -hypointensity reflects diffuse ferritin and Fe(3+) deposition, hyperintensity reflects tissue rarefaction. The HPR reflects degeneration of the putaminal lateral margin and/or external capsule. These findings reflect characteristic histological findings of MSA with parkinsonism.

We report on a four-year-old girl with head trauma caused by a motor vehicle accident. She presented with delirium, oculomotor palsy and ptosis in her left eye, left hemiparesis, and pyramidal signs in all extremities. Computed tomography on the day of admission showed diffuse cerebral edema with right-sided predominance. Magnetic resonance images on day 3 of admission showed lesions of diffuse axonal injury and contusion in the corpus callosum and right occipital and bilateral temporal lobes. There was a low-intensity lesion in the white matter of the right hemisphere on T2-weighted images, fluid-attenuated inversion recovery, T2()-weighted images, apparent diffusion coefficient maps and diffusion-weighted images. This low-intensity lesion disappeared by day 7, and a transient brain atrophy in the right hemisphere appeared on day 28. The low signal intensity in the cerebral white matter was apparently different from that associated with contusion and typical diffuse axonal injury, and might represent a late-onset accumulation of non-heme iron and free radicals in the white matter after head trauma.

The aim of this study is to evaluate the usefulness of diffusion-weighted (DW) magnetic resonance (MR) imaging in detecting peritoneal dissemination in cases of gynecological malignancy. We retrospectively analyzed MR images obtained from 26 consecutive patients with gynecological malignancy. Peritoneal dissemination was histologically diagnosed in 15 of the 26 patients after surgery. We obtained DW images and half-Fourier single-shot turbo-spin-echo images in the abdomen and pelvis, and then generated fusion images. Coronal maximum-intensity-projection images were reconstructed from the axial source images. Reader interpretations were compared with the laparotomy findings in the surgical records. Receiver-operating characteristic (ROC) curves were used to represent the presence of peritoneal dissemination. In addition, the sensitivity and specificity were calculated. DW imaging depicted the tumors in 14 of 15 patients with peritoneal dissemination as abnormal signal intensity. ROC analysis yielded Az values of 0.974 and 0.932 for the two reviewers. The mean sensitivity and specificity were 90 and 95.5%. DW imaging plays an important role in the diagnosis and therapeutic management of patients with gynecological malignancy.

Postmortem magnetic resonance (MR) images were correlated with the histological findings in two autopsy-proven cases of Wallerian degeneration of the corticospinal and corticopontine tracts associated with cerebral embolic infarction. T2 hyperintensities seen in Wallerian degeneration showed vacuolation of myelin in the early stage, and marked loss of myelin and axons with macrophages in the subacute and chronic stages. Similar T2 hyperintensities seen in the different stages of Wallerian degeneration reflect different histological findings.

A 6-month-old boy with persistent primitive trigeminal artery (PPTA) presented with stridor, dysphagia, delayed motor development and postural neck and shoulder dystonia. Magnetic resonance imaging/angiography and ultrasonography revealed PPTA, with flow from the dilated basilar artery to the right internal carotid artery, lower brainstem compression by the dilated basilar artery, and cerebellar vermis hypoplasia. Evoked potentials showed lower pons and medulla oblongata functional disruption. These lesions may be related to vascular etiology in the lower brainstem or to congenital malformation syndrome involving infratentorial structures. The relationship of this condition to Möbius syndrome is discussed.

Background Data about the long-term mortality of acute myocardial infarction (AMI) patients with renal insufficiency who received sufficient early revascularization are scant, so the present study evaluated the impact of serum creatinine levels on the long-term mortality in patients with AMI undergoing successful primary percutaneous coronary intervention (PCI). Methods and Results The Heart Institute of Japan Acute Myocardial Infarction (HIJAMI) registry has 3,021 consecutive AMI patients. Primary PCI was attempted in 1,451 patients and successful revascularization was obtained in 1,359 patients (93.6%). An elevated serum creatinine level, defined as creatinine ≥1.2 mg/dl, was observed in 216 patients (15.8%). Univariate analyses showed statistical differences between normal and elevated serum creatinine groups in age, gender, hypertension, previous myocardial infarction, number of diseased vessels and Killip class. During a median follow-up period of 39 [32-49] months, the event-free survival rate was lower in elevated creatinine group than normal creatinine group. Multivariate Cox proportional hazards model showed that serum creatinine level was an independent predictor of long-term mortality (adjusted hazard ratio 1.43 [95% confidence interval 1.03-1.99]). Conclusion The serum creatinine level on admission in patients with AMI predicts long-term mortality, even in those with successful primary PCI. (Circ J 2007; 71: 1354 - 1359)

We describe two cases of primary angiitis of the central nervous system in children (cPACNS) diagnosed by vessel wall contrast enhancement on magnetic resonance imaging (MRI). Both patients developed acute cerebral infarction after fever and malaise. In patient 1, a 7-month-old boy, MRI revealed extensive cerebral infarction in the right middle cerebral artery (MCA) area and stenosis at the M1 portion of the right MCA. Oral glucocorticoid therapy was initiated. Vessel wall enhancement was ameliorated 3months after onset, and stenosis was mostly restored. Patient 2, a 5-year-old boy, suffered from cerebral infarction in the left MCA area, and stenosis was identified in the left internal carotid artery, left MCA, and left posterior cerebral artery. Although vessel wall enhancement was reduced after glucocorticoid therapy, vessel wall enhancement of left MCA re-emerged, accompanied by increased erythrocyte sedimentation rate (ESR) and, decreased cerebral blood flow (CBF) in the affected hemisphere. Intravenous methylprednisolone therapy followed by oral glucocorticoid and mycophenolate mofetil resulted in resolution of these findings. Vessel wall enhancement is a promising finding in the diagnosis of cPACNS. Disease flares occur rarely in medium-to-large vessel cPACNS during dose tapering. Vessel wall enhancement, ESR, and CBF may be useful for the assessment of the activity of angiitis.

Chemoprevention of hepatocellular carcinoma (HCC) is one of the most challenging aspects of medical research. Vitamin K2 (VK2) has been suggested for its chemopreventive role in treatment of HCC, while inconsistent results in clinical trials have been reported. The present study was initiated to add to our insight into the anti-HCC cell proliferative effect of VK2 and its derivatives from a viewpoint of chemical structure. No significant effect was observed with original VK2, while VK2 derivatives bearing both isoprene units and a carboxyl-terminated side chain dose-dependently inhibited the growth of HCC cells without affecting normal liver cells. Loss-of-function analyses revealed that the anti-HCC cell activity by the VK2 derivatives was not mediated by a VK2 binding protein Bcl-2 homologous antagonist/killer (Bak) but rather associated with caspase/transglutaminase-related signaling pathways. Further studies on the carboxylic derivatives of VK2 bearing isoprene structural units introduced in this study might shed new light on the systemic treatment and prevention of HCC.

After practice, augmented feedback is the most important factor that facilitates motor learning. We assess the potential effectiveness of two types of augmented auditory feedback on the re-learning of arm reaching in individuals with stroke: (a) real-time knowledge of performance (KP) feedback and (b) rhythmic cueing in the form of knowledge of results (KR) feedback.Five participants with stroke underwent short-term practice, reaching with their affected arm with KP, KR and no feedback, on separate days. We assessed range of motion of the upper extremity (shoulder, elbow) and trunk, mean error and variability of the performed trajectory, and movement time, before and after training.All participants benefitted from practice with feedback, though the effects varied across participants and feedback type. In three participants, KP feedback increased elbow extension and reduced compensatory trunk flexion. In four participants, KR feedback reduced movement time taken to perform the reach. Of note, one participant benefitted mostly from KP feedback, which increased shoulder flexion and elbow extension, and decreased compensatory trunk flexion and mean error.Within day practice with augmented auditory feedback improves reaching in individuals with stroke. This warrants further investigation with longer practice periods in a larger sample size.After practice, augmented feedback is the second most important factor that facilitates motor learning. Music-based augmented auditory feedback has potential to enhance reaching abilities in individuals with stroke. Future studies are warranted to evaluate the long-term effectiveness of this feedback over a longer training period in a larger sample size.

Aim To delineate the clinical and neuroimaging characteristics of localized megalencephaly involving the right frontal lobe. Method Data from three patients aged 14–16 years at the last follow-up were retrospectively reviewed. Results All the patients were normal on neurological examination with no signs of hemiparesis. Enlargement of the right frontal lobe with increased volume of subcortical and deep white matter, as well as thickening of the ipsilateral genu of the corpus callosum was common. The onset of epilepsy was 4–7 years of age, with seizure types of massive myoclonus in two and generalized tonic-clonic in two, which could be eventually controlled by antiepileptics. Interictal electroencephalography showed frontal alpha-like activity in one, and abundant spike–wave complexes resulting in diffuse continuous spike–wave activity during sleep in two patients even after suppression of clinical seizures. Psychomotor development appeared unaffected or slightly delayed before the onset of epilepsy, but became mildly disturbed during follow-up period of 7–11 years. Conclusion Certain patients with right frontal megalencephaly can present with a milder epileptic and intellectual phenotype among those with localized megalencephaly and holohemispheric hemimegalencephaly, whose characteristic as epileptic encephalopathy was assumed from this study.

Purpose To determine whether fluorodeoxyglucose positron emission tomography (FDG-PET) before and after palliative radiation therapy (RT) can predict long-term pain control in patients with painful bone metastases. Methods and Materials Thirty-one patients with bone metastases who received RT were prospectively included. Forty painful metastatic treatment fields were evaluated. All patients had undergone pre-RT and post-RT PET/CT scanning. We evaluated the relationships between the pre-RT, post-RT, and changes in maximum standardized uptake value (SUV max ) and the pain response, and between SUV max and pain relapse of the bone metastases in the treatment field. In addition, we compared the SUV max according to the length of time from the completion of RT to pain relapse of the bone metastases. Results Regarding the pain response at 4 weeks after the completion of RT, there were 36 lesions of 27 patients in the responder group and 4 lesions of 4 patients in the nonresponder group. Changes in the SUV max differed significantly between the responder and nonresponder groups in both the early and delayed phases ( P =.0292 and P =.0139, respectively), but no relationship was observed between the pre-RT and post-RT SUV max relative to the pain response. The responder group was evaluated for the rate of relapse. Thirty-five lesions of 26 patients in the responder group were evaluated, because 1 patient died of acute renal failure at 2 months after RT. Twelve lesions (34%) showed pain relapse, and 23 lesions (66%) did not. There were significant differences between the relapse and nonrelapse patients in terms of the pre-RT (early/delayed phases: P P P =.0199/ P =.0261), and changes in SUV max ( P =.0004/ P =.004). Conclusions FDG-PET may help predict the outcome of pain control in the treatment field after palliative RT for painful bone metastases.

To investigate the difference in apparent diffusion coefficient (ADC) measurements of differently shaped regions of interest (ROIs) in ovarian tumors, and to investigate the diagnostic ability of differently shaped ROIs in differentiating benign from malignant ovarian tumors.Fifty-four patients with ovarian tumors with a solid component were evaluated. The patients underwent magnetic resonance (MR) examinations including diffusion-weighted imaging using a 3.0T MR system. Two readers measured ADCs using four ROI methods: freehand, square, round, and five small round ROIs. The interclass correlation coefficient (ICC) and repeated-measures analysis of variance were used to assess their measurement reliability and to compare ADCs for each ROI method. Receiver operating characteristic curve analysis and unpaired t-test on each ROI were used to differentiate benign and malignant ovarian tumors and assess the diagnostic ability.All ROI methods except the square ROI (0.56) showed good or excellent correlations (0.70-0.91). Minimum and mean ADC values differed significantly between the ROIs (P0.05). When using the freehand ROI, the minimum and mean ADC values were the lowest and highest, respectively. The optimal cutoff minimum and mean ADC values of each ROI for differentiating benign and malignant tumors were 0.81-1.06 × 10(-3) mm(2) /s and 1.15-1.52 × 10(-3) mm(2) /s, respectively. The areas under the curve showed no significant differences among the ADCs in the different ROI methods (P0.05). Minimum and mean ADCs from all ROIs showed significant differences between benign and malignant tumors (P0.05).The ROI shape influences ADC values and the optimal cutoff ADC values for differentiating benign from malignant ovarian tumors.

Molecular structure calculations indicated that the dibenzosilole skeleton could be well superposed on phenanthridinone, which is a structural component of ligands of retinoic acid receptor-related orphan receptors (RORs). Therefore, we designed, synthesized and biologically evaluated a series of novel ROR ligands based on the dibenzosilole scaffold as a hydrophobic core structure. Dibenzosilole derivatives bearing a hexafluoro-2-hydroxypropyl group on the benzene ring exhibited significant ROR-inhibitory activity, comparable to that of the lead phenanthridinone derivative 5. Our results indicate that the dibenzosilole skeleton would be a useful scaffold for developing novel biologically active compounds, and that cis-amide structure can be replaced by an alkylsilyl functionality.