标题：Design, synthesis and biological activities of thiourea containing sorafenib analogs as antitumor agents
作者机构：[Yao, J] Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan, Shandong 250012, Chin 更多
通讯作者地址：[Xu, WF]Shandong Univ, Dept Med Chem, Sch Pharmaceut Sci, 44 W Culture Rd, Jinan 250012, Shandong, Peoples R China.
来源：Bioorganic and medicinal chemistry
关键词：Antitumor agents;Diaryl thiourea;Sorafenib analogs;Synthesis
摘要：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 1H NMR, 13C 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.