肉桂酰氧基膦酸酯衍生物的合成与抗肿瘤活性

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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、~(13)C 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。 In order to find the anti-tumor lead compounds, 12 new compounds were designed and synthesized with cinnamoyl chloride and α-hydroxy phosphonate as raw materials under the aid of microwave irradiation. The results of IR, 1H NMR, 13 C NMR and elemental analysis Confirm the structure. The anti-tumor activity of the target compounds was tested by MTT assay. The results showed that these compounds had some inhibitory effects on the tumor cells. The inhibitory rate of SGC-7901 at 20μmol·L -1 Was 68.8%. The inhibitory rate of compound 3h on SGC-7901 was 48.0% at 5μmol·L -1, which showed good antitumor activity.
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