Chin. J. Org. Chem. ›› 2011, Vol. 31 ›› Issue (11): 1785-1798. Previous Articles     Next Articles




  1. (中国科学院上海药物研究所 新药研究国家重点实验室 上海 201203)
  • 收稿日期:2010-11-19 修回日期:2011-03-25 发布日期:2011-05-03
  • 通讯作者: 柳红

Fluorine in Medicinal Chemistry

WANG Jiang, LIU Hong   

  1. (State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sci-ences, Shanghai 201203)
  • Received:2010-11-19 Revised:2011-03-25 Published:2011-05-03
  • Contact: Hong Liu

Fluorinated compounds comprise a substantial proportion in the therapeutic drugs. It is an important strategy to introduce fluorine and fluorinated substitutes in the small molecule for structure-based medicinal chemistry. They can modulate the physicochemical and pharmacokinetic properties to improve bioavailability, alter the conformation of a molecule to enhance the selectivities and binding affinity to target proteins, and block metabolically labile sites to increase the metabolic stability of drugs.

Key words: fluorine, drug design, lead optimization