Design,Synthesis and Biological Activities of Quinazoline Containing Sorafenib Analogs as Antitumor Agents

作     者：ZHANG Jingwen WANG Ningning XIE Xiaoxia YAN Chunhong FU Fenghua YAO Jianwen WANG Hongbo 

作者机构：School of Pharmacy Yantai University Yantai 264005Shandong China GRU Cancer Center Georgia Regents University AugustaGA 30912 USA 

出 版 物：《Wuhan University Journal of Natural Sciences》 (武汉大学学报（自然科学英文版）)

年 卷 期：2017年第22卷第3期

页      面：239-246页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 100706[医学-药理学] 100602[医学-中西医结合临床] 10[医学] 

基　　金：Supported by the National Natural Science Foundation of China(81202038) Science and Technology Innovation Foundation in Yantai University(01081) 

主　　题：sorafenib analogs synthesis quinazoline antitumor agents 

摘      要：A series of novel sorafenib derivatives containing quinazoline moiety were designed and synthesized. Their anti-proliferative activities against HCT116 and HCT115 cell lines were evaluated using MTT assay. Most of the synthesized compounds showed significant cytotoxicity against the selected cell lines. These cytotoxicities were consistent with their inhibitory activity against the phosphorylation of c-Raf, MEK1/2 and ERK1/2. Compound GD-09 also showed much stronger anti-tumor activity than that of sorafenib in vivo by B16 melanoma xenograft model test.