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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Design, synthesis and biological evaluation of novel 4-thiazolidinones containing indolin-2-one moiety as potential antitumor agent.
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Design, synthesis and biological evaluation of novel 4-thiazolidinones containing indolin-2-one moiety as potential antitumor agent.

机译：设计，合成和生物学评估新型的4-噻唑烷酮类化合物，其中含有吲哚-2-酮部分作为潜在的抗肿瘤剂。

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摘要

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 (IC(50) = 0.025 muM, 0.075 muM, 0.77 muM, 1.95 muM) was 52, 36, 4.8 and 3.3 times more active than Sunitinib (IC(50) = 1.3 muM, 2.7 muM, 3.7 muM, 6.47 muM) against HT-29, H460, MDA-MB-231 and SMMC-7721 cancer cell line, respectively.
机译：设计并合成了一系列新型的4-噻唑烷酮和吲哚-2-酮杂合衍生物5a-5s和10a-10s，并在体外评估了它们对包括HT-29（人类结肠癌）在内的三种人类癌细胞系的细胞毒活性。 MTT分析法检测H460，H460（人肺癌），MDA-MB-231（人乳腺癌）。进一步针对一种癌细胞系SMMC-7721（人类肝癌）和一种正常细胞系WI-38（人类胎儿肺成纤维细胞）进一步评估了几种有效的目标化合物（5m，5p，5s，10a，10c-10g，10m，10p）。 ）。大多数制备的化合物对不同的人类癌细胞系均显示出显着的抗肿瘤活性。化合物10c（IC（50）= 0.025μM，0.075μM，0.77μM，1.95μM）的活性分别是舒尼替尼（IC（50）= 1.3μM，2.7μM，3.7μM，6.47μM）的52、36、4.8和3.3倍）分别针对HT-29，H460，MDA-MB-231和SMMC-7721癌细胞系。

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