卤素对核酸类药物的修饰与影响研究进展

doi:10.11944/j.issn.1000-0518.2018.05.170280

摘要/Abstract

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。

关键词: 卤素, 嘧啶, 嘌呤, 核糖, 修饰, 影响

Abstract:

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.

Key words: halogenation, pyrimidine, purine, ribose, modification, effects

陈行,刘春冬,王建华. 卤素对核酸类药物的修饰与影响研究进展[J]. 应用化学, 2018, 35(5): 491-499.

CHEN Hang,LIU Chundong,WANG Jianhua. Research Progress on Modification and Effects of Halogen on Nucleic Acid Drugs[J]. Chinese Journal of Applied Chemistry, 2018, 35(5): 491-499.

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