A novel series of indolin-2-one derivatives containing the 4-thiazolidinone moiety (5a-5p) was synthesized and the cytotoxicity of these derivatives was evaluated in vitro against three human cancer cell lines (HT-29, H460 and MDA-MB-231) by standard MTT assay. Some prepared compounds exhibited significant cytotoxicity against different human cancer cell lines. Several potent compounds were further evaluated against one normal cell line (WI-38). In particular, the promising compound 5h showed remarkable cytotoxicity and selectivity against the HT-29 and H460 cancer cell lines (IC(50) = 0.016 µmol/L, 0.0037 µmol/L, respectively).
In an attempt to develop potent antitumor agents, a series of novel 2-hydrazonylpyrido[2,3-b]pyrazin-3(4H)-one derivatives were designed and synthesized. All the prepared compounds were screened for their cytotoxic activities against A549, MDA-MB-231 and HT-29 cell lines in vitro. Pharmacological data indicated that five of the target compounds showed cytotoxicity against A549 cell line below a concentration of 1 µM. Compound 15g was the most potent one with IC(50) values of 0.19, 2.11 and 2.15 µM against A549, MDA-MB-231 and HT29 cell lines, respectively.
Most of the title compounds display moderate to excellent cytotoxic activities against one or more cancer cell lines. In particular, hybrides (IIIb) and (IVb) exhibit potent antitumor activity against all four cancer cell lines. -(WANG, S.; ZHAO, Y.; ZHANG, G.; LV, Y.; ZHANG, N.; GONG*, P.; Eur.
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