Abstract

A series of hybrids of 3-hydroxy-indolin-2-one and 2,3-dihydroquinolin-4(1H) -one were synthesized and their anti-proliferative activities against two human cancer cell lines were initially evaluated. Compound 7g was selected for further study and demonstrated moderate anti-proliferative activities against four human cancer cell lines. Meanwhile, 7g had inhibitory effects on the growth of SGC-7901 cells in dosage-and time-dependent manners and the cancer cells appeared morphological changes. Moreover, 7g was more effective in the inhibition of xenografted tumor in vivo growth and mice treated with 7g showed more weight gain than 5-FU-treated mice over the treatment period, suggesting a lower toxic effect than 5-FU. After treatment with 7g, the tumor showed typical morphological changes as evaluated by H&E staining.

Keywords: 3-Hydroxy-indolin-2-one, 2, 3-Dihydroquinolin-4(1H)-one, anticancer, hybrid, isatin, synthesis.

Graphical Abstract