Expeditious solvent-free synthesis of 1,3-thiazolanes via multicomponent reactions

A series of 1 3-thiazolane derivatives have been synthesized via multicomponent reactions of activated acetylenes,primary amines and isothiocyanates in the presence of a catalytic amount of Nmethylimidazole under solvent-free conditions.

Synthesis and antiproliferative activity of novel 4-substituted-phenoxy-benzamide derivatives

A series of novel 4-substituted-phenoxy-benzamide derivatives bearing an aryl cycloaliphatic amine moiety were synthesized and evaluated for antiproliferative activity against SW620, HT29 and MGC803 cancer cell lines in vitro. The pharmacological data demonstrated that the majority of target compounds exhibited moderate efficacy in HT29 and MGC803 cell lines. Compound 10 c showed promising inhibition of hedgehog（Hh） signaling pathway in an Hh-related assay. In addition, the superposition pattern of 10 c showed a good fit for a pharmacophoric model generated by Hh inhibitors and provided a basis for further structural optimization.

Chemoselective synthesis and cytotoxic activity of a series of novel benzo[1,4]oxazin-3-one derivatives

That tetraacetonitrile copper perchlorate catalyzes intramolecular amidation of arenes was found to be a new strategy for construction of nitrogen-containing heterocycles and resulted in the formation of a series of novel benzo[1,4]oxazin-3-one derivatives from N-（1,3-diphenyl-1H-1,2,4-triazol-5-yl）-2-phenoxyacetamides.This approach of heterocyclic construction proceeds in a chemoselective manner in which only benzo[1,4]oxazin-3-one derivatives were obtained by C—N bonds formation with cheap and simple copper salt catalyst under mild conditions in moderate to good yields.The biological assay of some of benzo[1,4]oxazin-3-one derivatives showed that they had moderate antiproliferative activity toward MDA-MB231 and HeLa cancer cell lines.