Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives Bearing Semicarbazone Moiety as Antitumor Agents  

作　　者：MA Junjie HU Gang XIE Lijun CHEN Lei XU Boxuan GONG Ping 

机构地区：[1]Key Laboratory of Structure-based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China [2]Fujian Institute of Microbiology, Fuzhou 350007, P. R. China

出　　处：《Chemical Research in Chinese Universities》2015年第6期958-963,共6页高等学校化学研究（英文版）

基　　金：Supported by the Program for Liaoning Excellent Talents in University, China（No.LR2014030） and the National Natural Science Foundation of China（No.81102470）.

摘　　要：A series of novel benzothiazole derivatives bearing semicarbazone as a linker was designed and synthe- sized, and their in vitro antitumor activities were evaluated against four cancer cell lines（HT29, H460, A549 and MDA-MB-231）. Most of them showed moderate to excellent activity against all the tested cell lines. Among them, compounds 12a--12i with fluoro-substituted benzyl-1H-indole moiety displayed more potent activity than those with phenyl moiety. The most promising compound 12d exhibited excellent antitumor activity with IC50 values of 0.015, 0.28, 1.53 and 0.68 p.mol/L against the four tested cell lines respectively.A series of novel benzothiazole derivatives bearing semicarbazone as a linker was designed and synthe- sized, and their in vitro antitumor activities were evaluated against four cancer cell lines（HT29, H460, A549 and MDA-MB-231）. Most of them showed moderate to excellent activity against all the tested cell lines. Among them, compounds 12a--12i with fluoro-substituted benzyl-1H-indole moiety displayed more potent activity than those with phenyl moiety. The most promising compound 12d exhibited excellent antitumor activity with IC50 values of 0.015, 0.28, 1.53 and 0.68 p.mol/L against the four tested cell lines respectively.

关 键 词：BENZOTHIAZOLE SEMICARBAZONE Antitumor activity 

分 类 号：O626.25[理学—有机化学] X826[理学—化学]