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Design and synthesis of isatin/triazole conjugates that induce apoptosis and inhibit migration of MGC-803 cells.

European Journal of Medicinal Chemistry(2016)

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摘要
A series of new isatin/triazole conjugates were designed based on the hypothesis that the ester-linked compounds could be enzymatically hydrolyzed by cellular esterases inside the cells. These compounds showed moderate to good growth inhibition toward the tested cancer cells, exerted selective inhibition toward MGC-803 cells and were less toxic to normal cells HL-7702 and GES-1. Of these compounds, compound 5a showed the best inhibitory activity against MGC-803 cells (IC50 = 9.78 μM), induced apoptosis through multiple mechanisms, as well as inhibited migration of MGC-803 cells.
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关键词
Isatin,Triazole,Cytotoxicity,Apoptosis,Migration inhibition,LSD1 inactivation
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