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A novel series of coumarin substituted thiazolyl-3-aryl-pyrazole-4-carbaldehydes ( 4a – o ) were synthesized via an efficient, one-pot multicomponent approach involving 3-(2-bromoacetyl)coumarins ( 1a – g ), thiosemicarbazide ( 2 ) and substituted acetophenones ( 3a – c ) utilizing Vilsmeier–Haack reaction condition with good yields. The title compounds structure was elucidated by spectroscopic data (IR, NMR and Mass) and elemental analysis. All the synthesized compounds were screened for their in vitro cytotoxic activity against MCF-7, DU-145 and HeLa cell lines and studied detailed about molecular interaction of probable target protein human microsomal cytochrome CYP450 2A6 using docking simulation. These coumarin derivatives were exhibiting moderate to appreciable cytotoxic activities. The compounds 4m and 4n exhibited significant cytotoxic activity with IC 50 values having 5.75 and 6.25 μM against HeLa cell line. Similarly compound 4n also exhibiting good anti cancer property and antibacterial activity against DU-145 cell line and Gram negative bacterial strains. [ABSTRACT FROM AUTHOR]

A series of new 3,6-diphenylimidazo[2,1- b ]thiazole derivatives ( 4a – l ) are synthesized and evaluated for their anticancer activity. Some of the synthesized compounds have shown potent anti-proliferative activity against HeLa, MDA-MB-231, A549 and THP1 human cancer cell lines. Among the active compounds, 3-(3-trifluoromethylphenyl)-6-phenylimidazo[2,1- b ]thiazole ( 4j ) has caused significant cytotoxicity in HeLa cells, with IC 50 as low as 6.5 μM. Compound 4j has induced caspase-3 and caspase-8 activation, leading to an apoptotic cell death. FACS analysis has revealed that compound 4j arrests cells in G0/G1 phase. The presence of 3-(3-trifluoromethylphenyl)- or 3-(3-chlorophenyl)-substituent, in that order, on the 6-phenylimidazo[2,1- b ]thiazole impacts more positively than other aryl-substituents, on the anti-proliferative properties of these compounds. [ABSTRACT FROM AUTHOR]

Abstract: A series of novel 1,2,3-triazole substituted N-phenyl nitrone derivatives 5a–e were prepared in three steps starting from 1-substituted-1,2,3-triazole-4-carbaldehydes 2 via Schiff's base formation, reduction followed by oxidation. Similarly, 1,2,3-triazole substituted N-alkyl nitrone derivatives 6a–p were prepared in single step starting from compound 2 on reaction with N-alkyl hydroxylamine hydrochlorides. All the final compounds were screened for anti-inflammatory and anticancer activity against various cancer cell lines. Among the compounds tested, the compounds 5a, 5d, 6a, 6b, 6m and 6o exhibited significant inhibition of IL-1β secretion as a measure of anti-inflammatory activity. Compound 5b, 5c, 6h, 6i and 6o exhibited significant activity against all the cell lines (A549, COLO 205, MDA-MB 231 and PC-3) at IC50 values of <15 μM. [Copyright &y& Elsevier]