Design, synthesis and biological evaluation of thiourea and nicotinamide-containing sorafenib analogs as antitumor agents

MedChemComm
2015.0

Abstract

A series of thiourea and nicotinamide-containing sorafenib analogs (7a-n) were designed and synthesized and their antiproliferative activities were tested against HCT116, MDA-MB-231, PC-3 and HepG2 cell lines. Most compounds showed potent activities against four cell lines, compound 7h showed better activities than sorafenib against all four cell lines, and compound 7a, 7e showed better activities against HCT116 and MDA-MB-231 cell lines. The anti-angiogenic activities of 7e and 7h are also better than that of sorafenib in both in vitro HUVEC tuber formation assay and ex vivo rat thoracic aorta rings assay.

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