喹诺酮羧酸酯衍生物的合成与生物活性

Synthesis and Bioactivities of Quinolone Derivates Containing Carboxylic Ester

摘要:

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3c、3g抗肿瘤活性最显著，在20 μ mol/L对 SGC-7901的抑制率分别为50.7 %、46.4 %。

Abstract:

In search of effective antitumor agents, According to substructure link principle, The quinolone compounds and α-hydroxyphosphonates were jogged. Eight O,O' - dialkyl - α - phenyl - α - substituted quinolinylanoxy methylphosphonate derivatives were designed and synthesized. The structures of all the compounds were confirmed by IR, NMR and elemental analysis. The bioassay of target compounds were tested. The result indicated that they exhibited certain antitumor activities. And compounds 3c, 3g showed obvious inhibition effect on SGC-7901 cells growth in vitro at 20 μ mol/L, inhibition ratio reached 50.7 %, 46.4 %, respectively.