Design, Synthesis and Antitumor Activity of Novel Indolin-2-one Derivatives Containing 4-Thiazolidinone Moiety  

作　　者：LIU Zijian HOU Yunlei ZHANG Guogang XU Ning MI Bin GONG Ping ZHAO Yanfang 

机构地区：[1]Key Laboratory of Structure-based Drug Design and D~covery, Min~try of Education, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China [2]State Key Laboratory Breeding Base-Hebei Province Key Laboratory of Molecular Chemistry for Drug, College of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang 050018, P. R. China

出　　处：《Chemical Research in Chinese Universities》2015年第2期235-243,共9页高等学校化学研究（英文版）

基　　金：Supported by the Program for Innovative Research Team of the Ministry of Education of China and the Program for Liaoning Innovative Research Team in University, China（No.IRT1073）, and the National Natural Science Foundation of China （No.81202405）

摘　　要：A series of novel indolin-2-one derivatives containing 4-thiazolidinone moiety（7a--7r） were synthesized and evaluated for their in vitro antitumour activities against MDA-MB-231 （human breast cancer）, H460（human lung cancer） and HT-29（human colon cancer） cell lines by standard 3-（4,5-dimethylthiazae-2-yl）-2,5-diphenyltetrazo- lium bromide（MTT） assay. Representative compounds（Td, 7k, 7m, 7p） with higher cytotoxicity were further examined against one normal cell line（WI-38, human fetal lung fibroblasts）. The preliminary investigation shows that most of the compounds display moderate to excellent potency and high selectivity against different human cancer cell lines. In particular, the most potent compound 7m shows promising cytotoxicity against MDA-MB-231, H460 and HT-29 cell lines with IC5o values of 0.78, 0.056 and 0.018 μmol/L, respectively. The potency is much higher than that of Sunitinib（IC50=3.46 μmol/L against MDA-MB-231, IC50=2.59 μmol/L against H460, IC50=1.50 μmol/L against HT-29） by 4.4, 46.3 and 83.3 fold.A series of novel indolin-2-one derivatives containing 4-thiazolidinone moiety（7a--7r） were synthesized and evaluated for their in vitro antitumour activities against MDA-MB-231 （human breast cancer）, H460（human lung cancer） and HT-29（human colon cancer） cell lines by standard 3-（4,5-dimethylthiazae-2-yl）-2,5-diphenyltetrazo- lium bromide（MTT） assay. Representative compounds（Td, 7k, 7m, 7p） with higher cytotoxicity were further examined against one normal cell line（WI-38, human fetal lung fibroblasts）. The preliminary investigation shows that most of the compounds display moderate to excellent potency and high selectivity against different human cancer cell lines. In particular, the most potent compound 7m shows promising cytotoxicity against MDA-MB-231, H460 and HT-29 cell lines with IC5o values of 0.78, 0.056 and 0.018 μmol/L, respectively. The potency is much higher than that of Sunitinib（IC50=3.46 μmol/L against MDA-MB-231, IC50=2.59 μmol/L against H460, IC50=1.50 μmol/L against HT-29） by 4.4, 46.3 and 83.3 fold.

关 键 词：lndolin-2-one 4-THIAZOLIDINONE Antitumour activity 

分 类 号：TQ455.47[化学工程—农药化工] O626[理学—有机化学]