羟基黄酮类化合物的合成及其抗肿瘤活性研究  

Study on Synthesis and Anti-tumor Activity of Hydroxyflavone Compounds

作　　者：冀学时[1] 王琳[1] 刘晓平[1] 胡春[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳10016

出　　处：《精细化工中间体》2012年第4期36-39,共4页Fine Chemical Intermediates

基　　金：国家自然科学基金资助项目(20474053)

摘　　要：设计合成了一系列羟基黄酮类化合物,并利用熔点、红外光谱、核磁共振氢谱和质谱确定了其结构。以利阿唑为阳性对照药,对4个目标化合物7-羟基黄酮、6-羟基黄酮、2′-甲氧基-6-羟基黄酮和2′-氯-6-羟基黄酮的抗HL-60活性进行了研究,实验结果表明2′-甲氧基-6-羟基黄酮,2′-氯-6-羟基黄酮均有较好活性,其中以2′-甲氧基-6-羟基黄酮的活性最显著,其半数抑制剂量为7.68μmol/L,与利阿唑活性相当。In order to study the influences of the position of hydroxyl and different substitution groups of hydroxyflavones on its anti-tumor activity,based on the structure-activity relationship reported,we designed and synthesized a series of hydroxyflavones and characterized with melting point,IR,H1 NMR and MS.The anti-tumor activities of four compounds in vitro were evaluated using HL-60.Results showed that 2'-methoxy-6-hydroxyl flavone and 2'-chloro-6-hydroxyl flavone exhibited potent anti-tumor activity.The anti-tumor activity of 2'-methoxy-6-hydroxyl flavone was significant with IC50 of 7.68 μm.

关 键 词：药物化学 羟基黄酮 合成 抗肿瘤活性 

分 类 号：TQ244[化学工程—有机化工]