期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 20, 期 9, 页码 2923-2929出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.03.018
关键词
Sorafenib analogs; Synthesis; Diaryl thiourea; Antitumor agents
资金
- National Science and Technology Major Project [2009-ZX09103-118]
- Ph.D. Programs Foundation of Ministry of Education of China [20110131110037]
A novel series of diaryl thiourea containing sorafenib derivatives 9a-t was designed and synthesized. The structures of all the newly synthesized compounds were determined by H-1 NMR, C-13 NMR and HRMS. Their antiproliferative activities against HCT116 and MDA-MB-231 cell lines, and their inhibitory activities against the phosphorylation of VEGFR were evaluated and described. Some of the compounds showed significant activities against both cell lines and VEGFR. Compounds 9g, 9m, 9o and 9p demonstrated competitive antiproliferative activities to sorafenib, the reference standard, while compounds 9d, 9m, and 9p showed significant inhibitory activities against the phosphorylation of VEGFR. (C) 2012 Elsevier Ltd. All rights reserved.
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