喹诺酮羧酸酯衍生物的合成与生物活性  

Synthesis and Bioactivity of Quinolone Derivates Containing Carboxylic Ester

作　　者：杨家强[1] 车万莉 马俊[1] 李明刚[1] 

机构地区：[1]遵义医学院药学院,贵州遵义563003

出　　处：《精细化工》2014年第4期463-466,共4页Fine Chemicals

基　　金：贵州省科技厅基金(黔科合J字LKZ[2010]47号)~~

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 search of effective antitumor agents and based on substructure link principle, the quinolone compounds and c^-hydroxyphosphonates were jogged and 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 the target compounds was tested. The results indicate that they exhibited certain antitumor activity. Among those compounds, m c and m g showed obvious inhibition effect on SGC -7901 cells growth in vitro at 20 μmol/L,and the inhibition ratio reached 50.7% and 46.4% ,respectively.

关 键 词：喹诺酮 α-羟基膦酸酯 生物活性 医药与日化原料 

分 类 号：R979.1[医药卫生—药品] R914.5[医药卫生—药学]