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

• Published in: Chemical research in Chinese universities 2015-04, Vol.31 (2), p.235-243
• Main Authors: Liu, Zijian, Hou, Yunlei, Zhang, Guogang, Xu, Ning, Mi, Bin, Gong, Ping, Zhao, Yanfang
• Format: Article
• Language: English
• Subjects: Analytical Chemistry; Anticancer properties; Biotechnology; Cancer; Chemistry; Chemistry and Materials Science; Chemistry/Food Science; Colon; Cytotoxicity; Derivatives; Fibroblasts; Inorganic Chemistry; Organic Chemistry; Physical Chemistry; Selectivity; Toxicity; 二氢; 体外抗肿瘤活性; 合成; 吲哚; 噻唑啉酮; 结构; 设计; 酮衍生物
• ISSN: 1005-9040; 2210-3171
• DOI: 10.1007/s40242-015-4335-8

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.