Design, Synthesis and Anticancer Activity of Novel 6-(Aminophenyl)-2,4-bismorpholino-1,3,5-triazine Derivatives Bearing Arylmethylene Hydrazine Moiety

doi:10.1007/s40242-014-3253-5

Abstract

Abstract:

In an attempt to develop potent and selective anticancer agents, we designed and synthesized a series of novel bis(morpholino-1,3,5-triazine) derivatives bearing aylmethylene hydrazine moiety and evaluated their cytotoxicity, in vitro, against H460(non-small-cell lung cancer), HT-29(human colorectal cancer) and MDA-MB-231(human breast cancer) cell lines. The pharmacological results indicate that all the compounds exhibit enhanced cytotoxicity than BMCL-200908069-1, and six target compounds(7e, 7h, 7j, 9a, 9b, 9c) were superior to PAC-1 against all the tested cancer cell lines. The most active compound 7j, with IC₅₀(inhibitory concentration 50%) values of 0.75, 0.34 and 0.60 μmol/L against HT-29, H460 and MDA-MB-231 cancer cell lines, was 39-, 28-, and 60-fold more potent than BMCL-200908069-1(29.24, 9.52 and 36.21 μmol/L), respectively.

Key words: Bis(morpholino-1,3,5-triazine), Design, Anticancer activity

HUANG Qiang, FU Qiangqiang, LIU Yajing, BAI Jinying, WANG Qianying, LIAO Huimin, GONG Ping. Design, Synthesis and Anticancer Activity of Novel 6-(Aminophenyl)-2,4-bismorpholino-1,3,5-triazine Derivatives Bearing Arylmethylene Hydrazine Moiety[J]. Chemical Research in Chinese Universities, 2014, 30(2): 257-265.

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