为了寻找抗肿瘤活性先导物,采用活性结构拼接原理,通过喹诺酮化合物与α-羟基膦酸酯拼合,设计合成8个O,O'-二烷基-α-苯基-α-取代喹啉甲酰氧基-甲基膦酸酯衍生物,经IR、NMR及元素分析进行结构确认。生物活性测试表明:该类衍生物对肿瘤细胞有一定增殖抑制作用,化合物Ⅲc、Ⅲg抗肿瘤活性最显著,在20μmol/L对SGC-7901的抑制率分别为50.7%、46.4%。 In order to find the precursor of anti-tumor activity, eight O, O'-dialkyl-α-phenyl-α-substituted quinolines A were designed and synthesized by the combination of quinolone compounds and α-hydroxy phosphonate The acyloxy-methyl phosphonate derivative was confirmed by IR, NMR and elemental analysis. The biological activity test showed that these derivatives have certain proliferation inhibitory effect on tumor cells. The compounds Ⅲc and Ⅲg have the most obvious antitumor activity. The inhibitory rates of SGC-7901 and 20μmol / L were 50.7% and 46.4% respectively.