Chinese Journal of Organic Chemistry ›› 2020, Vol. 40 ›› Issue (2): 300-326.DOI: 10.6023/cjoc201907055 Previous Articles     Next Articles


张芸溪, 高湖川, 张程瑞, 孙茂盛, 陈杨杰, 曾礼升, 黄岚, 陈鹏, 黄乾明, 蒲祥   

  1. 四川农业大学理学院 四川雅安 625014
  • 收稿日期:2019-07-31 修回日期:2019-10-20 发布日期:2019-11-07
  • 通讯作者: 蒲祥
  • 基金资助:

Advances in the Study of Structural Modification of Aspirin and Their Biological Activities

Zhang Yunxi, Gao Huchuan, Zhang Chenrui, Sun Maosheng, Chen Yangjie, Zeng Lisheng, Huang Lan, Chen Peng, Huang Qianming, Pu Xiang   

  1. College of Science, Sichuan Agricultural University, Ya'an, Sichuan 625014
  • Received:2019-07-31 Revised:2019-10-20 Published:2019-11-07
  • Supported by:
    Project supported by the National Natural Science Foundation of China (No. 21708028), the Education Department of Sichuan Province (No. 17ZA0301) and the Scientific Innovation Cultivation Project of Sichuan Province (No. 2018080).

Aspirin (ASP), the first synthetic drug, is widely used as a non steroidal anti-inflammatory drug. It displays a variety of biological activities, such as anti-thrombosis, anti-inflammatory, anti-tumor, etc. A lot of works about the synthesis and related activity evaluation of its derivatives were reported. There are four kinds of derivatization methods:skeleton derivatization, prodrug derivatization, twin derivatization and metal coordination derivatization. According to the different modification sites, skeleton derivatization could be further divided into C(1)-COOH site modification, C(1)-COOH site and C(2)-OAc site simultaneous modification, C(2)-OAc site modification and benzene ring modification. NO-ASP is the main method to prepare antithrombotic derivatives, and metal coordination modification is the main synthesis scheme of anticancer derivatives. The structure modification and bioactivity research of aspirin in recent twenty years and the synthetic routes of 353 aspirin derivatives and the pharmacological activities of some derivatives are described, which provides a reference for the further development of aspirin derivatives.

Key words: aspirin, skeleton derivation, prodrug derivation, twin drug derivation, metal coordination derivation