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

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 of the compounds showed potent activities against the four cell lines, compound 7h showed better activities than sorafenib against all four cell lines, and compounds 7a and 7e showed better activities against HCT116 and MDA-MB-231 cell lines. The anti-angiogenic activities of 7e and 7h were also better than that of sorafenib in both in vitro HUVEC tube formationassay and ex vivo rat thoracic aorta ring assay.