Chinese Journal of Applied Chemistry ›› 2018, Vol. 35 ›› Issue (5): 491-499.DOI: 10.11944/j.issn.1000-0518.2018.05.170280

• Review • Previous Articles     Next Articles

Research Progress on Modification and Effects of Halogen on Nucleic Acid Drugs

CHEN Hang,LIU Chundong,WANG Jianhua()   

  1. Bioengineering College of Chongqing University,Chongqing 400044,China
  • Received:2017-08-10 Accepted:2017-10-23 Online:2018-04-23 Published:2018-04-23
  • Contact: WANG Jianhua
  • Supported by:
    Supported by the Natural Science Foundation of Chongqing, China(No.Cstc2013jjB0011), the Social Programs and Human Security in Chongqing Science(No.Cstc2017shms-xdny0033), the Technology Innovation Projects(No.Cstc2017shms-xdny80006)


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