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Design,Synthesis and Antiproliferative Activities of Diaryl Thiourea Derivatives as Anticancer Agents
Authors:Jianwen Yao  Zuopeng He  Jing Chen  Daquan Chen  Wei Sun  Wenfang Xu
Affiliation:1. Department of Medicinal Chemistry, School of Pharmacy, Yantai University, Yantai, Shandong 264005, China;2. Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong 250012, China
Abstract:Two new series of diaryl thiourea containing sorafenib derivatives 9a – 9t were designed and synthesized, and their antiproliferative activities against PC‐3, HCT116 and MDA‐MB‐231 cell lines were evaluated. All compounds generally showed antiproliferative activity to PC‐3 cells, most of the analogs exhibited potent antiproliferative activity to HCT116 cells, and compounds 9e , 9f , 9o and 9p demonstrated inhibitory activities against all three cell lines. The structures of all the newly synthesized compounds were determined by 1H NMR, 13C NMR and HRMS.
Keywords:sorafenib analogs  diaryl thiourea  structure‐activity relationships  antiproliferative activity
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