蒽环类化合物的结构修饰及抗肿瘤活性研究进展  

Advances in Study of Structural Modification and Antitumor Activities of Anthracyclines

作　　者：赵越[1,2] 李怀业[1,2] 袁兰[2] 张殊佳[1] 

机构地区：[1]大连大学环境与化学工程学院,辽宁大连116622 [2]北京大学医药卫生分析中心,北京100191

出　　处：《中国药学杂志》2016年第12期953-961,共9页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金资助项目(91330103)

摘　　要：蒽环类化合物普遍具有抗肿瘤活性,是临床上使用的一类广谱抗肿瘤抗生素,但有些化合物具有较大的毒性和耐药性,由此限制了该类化合物的进一步发展和应用,而采取对该类化合物的结构进行修饰和改造,是解决这些问题较为有效的途径。因此,人们通过全合成或半合成等各种方法,研究与开发新型蒽环类化合物药物,以期找到疗效更好的蒽环类抗肿瘤药物。笔者在结合自己的工作和参考国内外文献基础上,简要介绍蒽环类化合物的作用机制、耐药性和心脏毒性,主要综述蒽环类化合物A环、糖基以及孪药蒽环类化合物的构效关系,为将来新型蒽环类化合物研发提供参考。Anthracyclines generally possess antitumor activities and they are clinically broad-spectrum anticancer antibiotics.But some of them have prominent toxicities and drug resistances.These limit their further development and applications.However,proper structural modifications can sometimes solve these problems.So lots of new anthacyclines are obtained through total-synthesis or partial-synthesis for the purpose of finding more effective new drugs.In this paper,combing with our previous work and referring the literatures,we briefly introduce the mechanism,drug resistance,cardiac toxicity of anthracycline,and mainly review the structure-activity relationships of ring A,sugar moieties and twin drugs of anthracyclines.These can provide powerful evidence for further developments of new anthracyclines.

关 键 词：蒽环化合物 结构修饰 抗肿瘤活性 

分 类 号：R282[医药卫生—中药学]