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根据活性片段组合原理,设计、合成了一系列新型E-2,3-二芳基丙烯酰氧基膦酸酯衍生物,结构经IR、1H NMR、13C NMR及元素分析确证。采用MTT法测试目标化合物的抗肿瘤活性。结果表明:部分化合物对于所测试肿瘤细胞有抑制作用,其中化合物3e对A-549的活性[IC50=(12.7±1.9)μmol·L-1]最为突出,与对照药顺铂[IC50=(8.0±1.5)μmol·L-1]较为接近;化合物3g、3k对EC-109的增殖抑制作用最好,IC50分别为(9.5±1.8)μmol·L-1和(11.5±0.9)μmol·L-1;化合物3i、3k对SGC-7901、A-549、EC-109三种肿瘤细胞均有较好抑制作用。该类衍生物值得进一步研究。
A series of novel derivatives of E-2,3-diarylacryloyloxy phosphonate were designed and synthesized according to the principle of active fragment assembly. The structures were confirmed by IR, 1H NMR, 13C NMR and elemental analysis. The antitumor activity of the target compound was tested by MTT assay. The results showed that some of the compounds showed inhibitory effect on the tumor cells tested. Among them, the activity of compound 3e against A-549 [IC50 = (12.7 ± 1.9) μmol·L-1] was most prominent compared with the control drug cisplatin [IC50 = (8.0 ± 1.5) μmol·L-1]. Compounds 3g and 3k had the best inhibitory effect on the proliferation of EC-109 with IC50 of (9.5 ± 1.8) μmol·L-1 and (11.5 ± 0.9) μmol·L- 1; Compounds 3i, 3k had better inhibitory effect on SGC-7901, A-549 and EC-109 tumor cells. Such derivatives deserve further study.