Synthesis and Antitumor Activity of Sorafenib Analogs Containing a Tetrazole Moiety  

作　　者：TIAN Ye YU Simiao CAI Lude GONG Guowei WU Guodong QI Hongxia ZHAO Yanfang QIN Mingze 

机构地区：[1]Key Laboratory of Structure-based Drug Design and Discovery,Ministty of Education Shenvang Pharmaceutical University,Shenyang 110016,P.R.China [2]Department of Bioengineering,Zhuhai Campus of Zunyi Medical University, Zhuhai 519041,P.R.China [3]Shengjing Hospital of China Medical University,Shenyang 110016,P.R.China

出　　处：《Chemical Research in Chinese Universities》2019年第1期41-46,共6页高等学校化学研究（英文版）

基　　金：the National Natural Science Foundation of China(No.81502924).

摘　　要：A novel series of diaryl biuret derivatives containing a tetrazole moiety was designed and synthesized.All the target compounds were evaluated for their in vitro antitumor activity against HT-29,HepG2,MCF-7 and A549 cells by MTT assay.Most of them exhibited obvious antitumor activity,and four of them(4a,4c,4h and 7a)were superior to sorafenib in general.Among them,Compound 4h displayed more potent activity than sorafenib in all tested cancer cells.Compound 4c exhibited the most outstanding activity in inhibition of growth of HepG2 cells(IC50=0.55 μmol/L).Further,they both revealed favorable metabolic stability in in vitro assay.Compounds 4c and 4h are promising candidates for further development.

关 键 词：SORAFENIB DERIVATIVE TETRAZOLE MOIETY ANTITUMOR activity 

分 类 号：O6[理学—化学]