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为了寻找新型抗肿瘤先导物,采用缩合剂N,N’-二环己基碳二亚胺(DCC)合成酯的方法,以O,O’-二烷基-1-羟基-(取代苯基)甲基膦酸酯、取代苯甲酸为原料合成16个目标物,其中12个化合物未见报道.经IR,1H NMR,13C NMR及元素分析对所合成的化合物进行了结构确认和表征.并首次研究了该系列化合物的抗肿瘤活性.结果表明:目标物具有一定的抑制肿瘤细胞增殖作用,其中2i,2k,2m对SGC-7901的IC50值分别为18.8,18.5,24.5μmol/L,对A-549的IC50值分别为24.1,29.0,20.7μmol/L,显示出潜在的抗肿瘤活性,值得进一步研究.在此基础上,初步研究其构效关系.
In order to find a new antitumor leader, a method of synthesizing an ester with a condensing agent N, N’-dicyclohexylcarbodiimide (DCC) was developed using O, O’-dialkyl-1- hydroxy- Methylphosphonates and substituted benzoic acids were used to synthesize 16 target compounds, of which 12 compounds were not reported.The structures of the synthesized compounds were confirmed by IR, 1H NMR, 13C NMR and elemental analysis, The antitumor activities of the compounds were studied. The results showed that the target compounds could inhibit the proliferation of tumor cells. The IC50 values of 2i, 2k and 2m against SGC-7901 were 18.8, 18.5 and 24.5μmol / L, respectively, The IC50 value of -549 was 24.1, 29.0 and 20.7 μmol / L, respectively, which showed potential antitumor activity and deserved to be further studied. On this basis, the structure-activity relationship was preliminary studied.