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 ...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.展开更多
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）
文摘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.
