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Using the robust N -heterocyclic carbene-palladium complex (SIPr) Ph2 Pd(cin)Cl, a highly efficient and easy-to-operate method has been developed at room temperature for the solvent-free Buchwald-Hartwig amination of heteroaryl chlorides with various amines. The amount of catalyst can be as low as 0.05 wt %. The system was demonstrated on 47 substrates and successfully applied to the synthesis of commercial pharmaceuticals and candidate drugs with high yields. Furthermore, the protocol can be used to prepare aniline derivatives on a multigram scale without yield loss.

The copper(ii)-catalyzed (4+1) cyclizations and copper(i)-catalyzed (3+2) cycloadditions of iodonium ylides and alkynes were successfully developed by employing efficient and safe iodonium ylides instead of traditional diazo compounds. Highly functionalized dimethyl (E)-3-benzylideneindoline-2,2-dicarboxylates and methyl 5-(2-hydroxyphenyl)-2-methoxy-4-phenylfuran-3-carboxylates were conveniently prepared in moderate to excellent yields. The possible reaction mechanisms were also discussed.

Multiple myeloma (MM) is characterized by abnormal proliferation of neoplastic plasma cells. Pleural effusion as an initial presentation of this disease is rare, as is true pleural myeloma. We herein present a case of solitary pleural myelomatous lesion in a 70-year-old male patient diagnosed by pleural biopsy via semi-rigid thoracoscopy followed by histopathological examination. Furthermore, a review of the related English literature identified 22 cases of pleural myeloma, only 3 of which were diagnosed by video-assisted thoracoscopy. To the best of our knowledge, this is the first reported case of a solitary pleural myelomatous lesion diagnosed by pleural biopsy via semi-rigid thoracoscopy. Patients with MM with pleural involvement, including the present case, appear to have a short survival despite aggressive treatment. Our patient received chemotherapy with bortezomib, epiadriamycin and dexamethasone; however, he deteriorated rapidly after one cycle of chemotherapy and succumbed to the disease 8 weeks after the initial presentation. According to our experience, semi-rigid thoracoscopy is an effective and safe method for obtaining a pleural specimen for histopathological evaluation.

Through the strategy to enhance the bulkiness on both the backbone and the N-aryl moieties, we designed and synthesized a type of bulky α-diimine palladium complex (i.e., {[Ar-N[double bond, length as m-dash]C(R)-C(R)[double bond, length as m-dash]N-Ar]PdCl2, (Ar = 2-benzhydryl-4,6-dimethylphenyl)}, C1, R = H; C2, R = An; C3, R = Ph). The structures of these palladium complexes were well characterized, while C1 and C3 were further characterized by X-ray diffraction. The catalytic performances of the precatalysts were screened for direct C-H bond arylation of heteroarenes. The bidentate N,N-palladium complex C3 with both a backbone and N-aryl bulkiness was found to be a highly efficient precatalyst under aerobic conditions. With a low palladium loading of 0.5-0.1 mol%, a variety of heteroarenes with challenging bulky steric aryl bromides as well as heteroaryl bromides are all applicable for this cross-coupling reaction.

A 36-year-old female presented with an eosinophilic pleural effusion. The eosinophilic pleural effusion was considered to have been caused by a parasitic infection. Spirometra mansoni spargana was confirmed by semi-rigid thoracoscopy. About 2 months after treatment with praziquantel for 3 days, the pleural effusion had disappeared on the chest roentgenogram., (Copyright © 2015 The Authors. Published by Elsevier Ltd.. All rights reserved.)

Small interfering RNA (siRNA) provides a promising therapeutic approach in the silencing of disease-causing genes. In the present study, the use of 2'-O-methyl-modified siRNA-cluster of differentiation 31 (siRNA CD31 ), with cationic liposome RNA interference (RNAi)-mate as a carrier, effectively silenced the platelet endothelial cell molecule 1 (PECAM-1) gene of murine hemangioendothelioma cells in vitro. In vivo , 2'-O-methyl-modified siRNA CD31 carried by RNAi-mate was successfully delivered, targeting the PECAM-1 gene in the vasculature of nude mouse lung carcinoma xenografts. The growth of the lung carcinoma xenografts was inhibited by the 2'-O-methyl-modified siRNA CD31 and RNAi-mate complexes, and the expression of the PECAM-1 protein was downregulated, with a simultaneous decrease in vascular endothelial growth factor (VEGF) protein in the lung carcinoma xenografts. 2'-O-methyl-modified siRNA CD31 -RNAi-mate complexes may provide a potential therapeutic strategy in lung carcinoma treatment. The effect of PECAM-1 on VEGF expression may possibly be attributed to the function of PECAM-1 signal transduction.

The objective was to investigate the molecular mechanism of mitochondrial reactive oxygen species (ROS) signaling regulation of pulmonary artery endothelial cell (HPAEC) secretion in the condition of oxidative stress. Acrolein (40 μM) induced HPAEC mitochondrial generation of ROS, rotenone (2 μmol/L) blocked mitochondrial respiratory chain complex I, cesium chloride (CsCl, 40 mmol/L)blocked K(+)channels, and saline (0.9 g/dl) were used as control. The generations of NOS, ET-1 and VEGF were determined with ELISA in the condition of different treatment reagents namely acrolein, acrolein plus rotenone, acrolein plus CsCl and saline. In the different reagent treatment of HPAECs, acrolein increased mitochondrial ROS, membrane potential, Kv1.5 mRNA and protein expression, intracellular calcium and the generation of NOS (determining NO production), ET-1 and VEGF, and those were reduced by rotenone. CsCl decreased the increment of membrane potential, the elevation of intracellular calcium and the upregulation of NOS, E-1 and VEGF expressions, which were induced by acrolein. The present study demonstrated that mitochondrial ROS-K(+)channel regulated HPAEC secretion of NO, ET-1 and VEGF in the condition of oxidative stress. Kv1.5 channel may be an important component of ROS-K+ channel signaling pathway, and intracellular calcium contributed to mitochondrial ROS-K(+) channel signaling modulation of HPAEC secretion.