摘要
药物分子中引入卤素具有改善药物脂溶性、影响药物分子的电荷分布及影响药物的作用时间等特点,故被广泛应用。作为抗病毒、抗肿瘤、干扰素诱导和免疫增强的、具有特定碱基序列的核酸药物也不例外。本文综述了卤素对核酸结构中的嘧啶类、嘌呤类和核糖结构修饰后的核酸类药物生物活性产生的影响,以期为核酸及核酸类似物的药物研发提供新的思路。
The halogenation is an invaluable approach for structural modification of drugs in medicine chemistry development. It increases the lipo-solubility, influences on the space charge distribution and improves their drug metabolic activity. Nucleic acid,as antiviral agent,antitumor agent,interferon inducer and immunopotentiator,can also be modified by halogenation. In this review we will discuss the effect on the bioactivity of modified nucleic acids on pyrimidines,purines and ribose by halogenation,and summarize the latest developments in drug research and development of modified nucleic acid.
作者
陈行
刘春冬
王建华
CHEN Hang;LIU Chundong;WANG Jianhua(Bioengineering College of Chongqing University, Chongqing 400044, Chin)
出处
《应用化学》
CAS
CSCD
北大核心
2018年第5期491-499,共9页
Chinese Journal of Applied Chemistry
基金
重庆市自然科学基金重点项目(Cstc2013jjB 0011)
重庆市社会事业与民生保障科技创新专项(Cstc2017shms-xdny0033)
重庆市社会事业与民生保障科技创新专项(Cstc2017shms-xdny80006)资助课题~~
关键词
卤素
嘧啶
嘌呤
核糖
修饰
影响
halogenation
pyrimidine
purine
ribose
modification
effects
