摘要
萘酰亚胺类化合物作为细胞探针、DNA靶向剂和抗肿瘤药物是当前药物领域的研究热点之一,先后有氨萘非特、双萘法德等多种衍生物进入了临床试验,但受限于毒性,未能进入市场。本文综述了单、双萘酰亚胺的设计开发过程,并对萘酰亚胺的结构与抗肿瘤活性之间的关系进行了分析总结,发现多种结构修饰对提高抗肿瘤活性、减少毒性具有意义。
The development of naphthalimide derivatives as cellular chemical probes,DNA targeting agents and antitumor drugs is one of the research hotspots in the current pharmaceutical field. Various naphthalimide derivatives such as amonafide and bisnafide have been used in clinical trials,but not yet entered the market due to their toxicity. In this paper,the development process of mono-and bis-naphthalimide is reviewed,and the relationship between the structure and antitumor activity of naphthalimides is also summarized and discussed. It is found that various structural modifications show an effect on improving antitumor activity and reducing toxicity.
作者
张海洋
齐秀丽
陈高云
ZHANG Hai-yang;QI Xiu-li;CHEN Gao-yun(Institute of Chemical Defence,Beijing 102205,China;The 74th Army Hospital,Guangzhou 510310,China)
出处
《国际药学研究杂志》
CAS
北大核心
2020年第1期8-15,21,共9页
Journal of International Pharmaceutical Research
关键词
萘酰亚胺类
DNA嵌合剂
抗肿瘤药物
构效关系
naphthalimides
DNA intercalator
antitumor
structure-activity relationship
