Design, synthesis and biological evaluation of novel 4-thiazolidinones containing indolin-2-one moiety as potential antitumor agent

作者：Wang, Shuobing; Zhao, Yanfang; Zhang, Guogang; Lv, Yingxiang; Zhang, Ning; Gong, Ping^*

来源：European Journal of Medicinal Chemistry, 2011, 46(8): 3509-3518.

DOI：10.1016/j.ejmech.2011.05.017

• 4-thiazolidinone
• Indolin-2-one
• Synthesis
• Cytotoxic activities

A series of novel 4-thiazolidinone and indolin-2-one hybrid derivatives 5a-5s and 10a-10s have been designed and synthesized and their cytotoxic activities were evaluated in vitro against three human cancer cell lines including HT-29 (human colon cancer), H460 (human lung cancer), MDA-MB-231 (human breast cancer) by MTT assay. Several potent target compounds (5m, 5p, 5s, 10a, 10c-10g, 10m, 10p) were further evaluated against one cancer cell line SMMC-7721 (human liver cancer) and one normal cell line WI-38 (human fetal lung fibroblasts). Most of the prepared compounds exhibited significant antitumor activities against different human cancer cell lines. Compound 10c (IC50 = 0.025 mu M. 0.075 mu M, 0.77 mu M, 1.95 mu M) was 52, 36, 4.8 and 3.3 times more active than Sunitinib (IC50 = 1.3 mu M, 2.7 mu M, 3.7 mu M, 6.47 mu M) against HT-29, H460, MDA-MB-231 and SMMC-7721 cancer cell line, respectively.

• 出版日期2011-8
• 单位沈阳药科大学