杨家强, 雷静, 黎刚, 万小强. 肉桂酰氧基膦酸酯衍生物的合成与抗肿瘤活性J. 药学学报, 2016,51(3): 420-424. doi: 10.16438/j.0513-4870.2015-0810
引用本文: 杨家强, 雷静, 黎刚, 万小强. 肉桂酰氧基膦酸酯衍生物的合成与抗肿瘤活性J. 药学学报, 2016,51(3): 420-424. doi: 10.16438/j.0513-4870.2015-0810
YANG Jia-qiang, LEI Jing, LI Gang, WAN Xiao-qiang. Synthesis and antitumor activity of cinnamoyloxy phosphonate derivativesJ. Acta Pharmaceutica Sinica, 2016,51(3): 420-424. doi: 10.16438/j.0513-4870.2015-0810
Citation: YANG Jia-qiang, LEI Jing, LI Gang, WAN Xiao-qiang. Synthesis and antitumor activity of cinnamoyloxy phosphonate derivativesJ. Acta Pharmaceutica Sinica, 2016,51(3): 420-424. doi: 10.16438/j.0513-4870.2015-0810

肉桂酰氧基膦酸酯衍生物的合成与抗肿瘤活性

Synthesis and antitumor activity of cinnamoyloxy phosphonate derivatives

  • 摘要: 为了寻找抗肿瘤先导化合物,在微波辅助下,以肉桂酰氯与α-羟基膦酸酯为原料,设计合成了12个新化合物,经IR、1H NMR、13C NMR及元素分析进行结构确认。采用MTT法对目标化合物进行体外抗肿瘤活性测试,结果表明:该类衍生物对所测肿瘤细胞有一定增殖抑制作用,其中化合物3c在20μmol·L-1下对SGC-7901抑制率为68.8%,化合物3h在5μmol·L-1下对SGC-7901抑制率达48.0%,有较好的抗肿瘤活性。

     

    Abstract: In search of more effective anticancer agents, twelve compounds were designed and synthesized via microwave-assisted reactions of cinnamoyl chloride with α-hydroxyphosphonate. The structures of all the compounds were confirmed by IR, NMR and elemental analysis. Bioassay of the compounds were tested. They exhibited certain antitumor activities. Especially, compound 3c had obvious inhibitory effect on growth of SGC-7901 cells in vitro at 20 μmol·L-1, and compound 3h showed better inhibitory effect on growth of SGC-7901 cells in vitro at 5 μmol·L-1, the inhibition ratio were 68.8% and 48.0%, respectively.

     

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