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Here, we report on the synthesis of libraries of new 5-arylidene-2-thioxo-1,3-thiazolidin-4-ones 3 (twenty-two compounds) and new 2-amino-5-arylidene-1,3-thiazol-4(5 H )-ones 5 (twenty-four compounds) with stereo controlled Z -geometry under microwave irradiation. The 46 designed final compounds were tested in order to determine their activity against four representative protein kinases (DYR1A, CK1, CDK5/p25, and GSK3α/β). Among these 1,3-thiazolidin-4-ones, the molecules (5 Z ) 5-(4-hydroxybenzylidene)-2-thioxo-1,3-thiazolidin-4-one 3e (IC 50 0.028 μM) and (5 Z )-5-benzo[1,3]dioxol-5-ylmethylene-2-(pyridin-2-yl)amino-1,3-thiazol-4(5 H )-one 5s (IC 50 0.033 μM) were identified as lead compounds and as new nanomolar DYRK1A inhibitors. Some of these compounds in the two libraries have been also evaluated for their in vitro inhibition of cell proliferation (Huh7 D12, Caco2, MDA-MB 231, HCT 116, PC3, and NCI-H2 tumor cell lines). These results will enable us to use the 1,3-thiazolidin-4-one core as pharmacophores to develop potent treatment for neurological or oncological disorders in which DYRK1A is fully involved.

Background: Oligodendroglioma is a rare type of primary brain tumor which, like other malignant gliomas, metastasizes very rarely even when in high-grade form., Case Report: A 36-year-old white man diagnosed 29 months previously as having 1p/19q codeleted anaplastic oligodendroglioma presented bilateral cruralgia and lower limb motor deficits. A computed tomography scan showed multiple osteoblastic bone lesions. The presence of oligodendroglial cells was revealed by bone marrow biopsy and confirmed by immunohistochemical analyses. A positon emission tomography-computed tomography scan confirmed the exclusive involvement of bones., Conclusion: This case joins less than 20 other reported cases of oligodendroglioma bone marrow metastasis, and is one of only a handful of cases of diffuse bone metastases beyond the axial skeleton. To the best of our knowledge, the early relapse of 1p/19q codeleted anaplastic oligodendroglioma with this distribution of metastases has never been described in the literature.

We here disclosed a new protocol for the condensation of acetophenone derivatives and active methylene compounds with aldehydes in the presence of boric acid under microwave conditions. Implementation of the reaction is simple, healthy and environmentally friendly owing to the use of a non-toxic catalyst coupled to a solvent-free procedure. A large variety of known or novel compounds have thus been prepared, including with substrates bearing acid or base-sensitive functional groups.

Purpose: To analyze the outcome and dose distribution of intensity-modulated radiation therapy (IMRT) by helical tomotherapy in women treated for large supradiaphragmatic Hodgkin's disease., Material and Methods: A total of 13 patients received adjuvant radiation at a dose of 30 Gy to the initially involved sites with a boost of 6 Gy to those areas suspected of harboring residual disease on the simulation CT scan., Results: With a median follow-up of 23 months, the two-year progression-free survival was 91.6%, and the 2- and 3-year overall survivals were 100%. We did not report any heart or lung acute side effects. The conformity index of PTV (Planning Target Volume) was better for IMRT than for 3D-CRT (p=0.001). For the breasts, lungs, heart, thyroid and esophagus, the volume distributions favored the IMRT plans. For the breasts, the V(20Gy), V(25Gy) and V(30Gy) were 1.5, 2.5 and 3.5 times lower, respectively, for IMRT than for 3D-CRT. For the lung tissues, the V(20Gy) and V(30Gy) were 2 times and 4.5 times lower, respectively, for IMRT than for 3D-CRT. For the heart, the V(20Gy) and V(30Gy) were 1.4 and 2 times lower, respectively, for IMRT than for 3D-CRT. For the esophagus, the V(35Gy) was 1.7 lower for IMRT than for 3D-CRT, and for the thyroid, the V(30Gy) was 1.2 times lower for IMRT., Conclusion: IMRT by helical tomotherapy improved the PTV coverage and dramatically decreased the dose in organs at risk. The treatment was well tolerated, but a longer follow-up is necessary to prove a translation of these dosimetric improvements in the outcome of the patients.

A practical protocol for the preparation of (5Z)-2-alkylthio-5-arylmethylene-1-methyl-1,5-dihydro-4H-imidazol-4-one derivatives is reported. The new compounds were obtained in good yield and stereoselectivity in two steps, namely a solvent-free Knoevenagel condensation under microwave irradiation, followed by an S-alkylation reaction with various halogenoalkanes.