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

Abstract：

: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 μM, 0.075 μM, 0.77 μM, 1.95 μM) was 52, 36, 4.8 and 3.3 times more active than Sunitinib (IC(50) = 1.3 μM, 2.7 μM, 3.7 μM, 6.47 μM) against HT-29, H460, MDA-MB-231 and SMMC-7721 cancer cell line, respectively.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Wang S,Zhao Y,Zhang G,Lv Y,Zhang N,Gong P

doi

10.1016/j.ejmech.2011.05.017

subject

Has Abstract

pub_date

2011-08-01 00:00:00

pages

3509-18

issue

8

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(11)00379-5

journal_volume

46

pub_type

杂志文章

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