Synthesis and Antitumor Activity of 4-tert-Butyl-5-benzyl-2-benzyliminothiazoles  

作　　者：YE Jiao QIU Shenyi HU Aixi PENG Junmei QIN Zhi 

机构地区：[1]College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, P. R. China

出　　处：《Chemical Research in Chinese Universities》2014年第1期49-54,共6页高等学校化学研究（英文版）

基　　金：Supported by the National Science ＆ Technology Pillar Program of China（No.2011BAE06B01） and the Natural Science Foundation of Hunan Province, China（No. 12j j3012）.

摘　　要：A series of novel Schiff bases including 4-tert-butyl-5-benzyl-2-benzyliminothiazoles was synthesized by reacting the aromatic aldehydes with the corresponding 2-aminothiazoles.The antitumor bioassay revealed that compounds 2n and 2m exhibited potent cytotoxicity against human cervix cancer（HeLa） cell line with IC50 values of 0.001 and 0.007 mmol/L,respectively.The preliminary structure-activity relationship（SAR） investigations and the apoptosis evaluation suggest that 4-tert-butyl-5-benzyl-2-benzyliminothiazoles may be a satisfactory backbone for antitumor activity,and compound 2n can serve as an attractive candidate for the development of novel apoptosis in anticancer treatment.A series of novel Schiff bases including 4-tert-butyl-5-benzyl-2-benzyliminothiazoles was synthesized by reacting the aromatic aldehydes with the corresponding 2-aminothiazoles.The antitumor bioassay revealed that compounds 2n and 2m exhibited potent cytotoxicity against human cervix cancer（HeLa） cell line with IC50 values of 0.001 and 0.007 mmol/L,respectively.The preliminary structure-activity relationship（SAR） investigations and the apoptosis evaluation suggest that 4-tert-butyl-5-benzyl-2-benzyliminothiazoles may be a satisfactory backbone for antitumor activity,and compound 2n can serve as an attractive candidate for the development of novel apoptosis in anticancer treatment.

关 键 词：2-AMINOTHIAZOLE Schiff base Antitumor activity 

分 类 号：TQ463.5[化学工程—制药化工] O625.312[理学—有机化学]