Journal of Chinese Pharmaceutical Sciences ›› 2022, Vol. 31 ›› Issue (1): 55-67.DOI: 10.5246/jcps.2022.01.006

• Original articles • Previous Articles     Next Articles

Design, synthesis, and biological evaluation of a series of novel cordycepin derivatives

Lijuan Jiang2, Tingting Cao1, Ruoyi Yang1, Ying Li1, Lin Dong1, Shufan Yin1,*()   

  1. 1 College of Chemistry, Sichuan University, Chengdu 610064, Sichuan, China
    2 School of Chemistry and Chemical Engineering, Guangxi University for Nationalities; Guangxi Key Laboratory for Polysaccharide Materials and Modifications, Nanning 530008, China
  • Received:2021-07-17 Revised:2021-08-11 Accepted:2021-09-16 Online:2022-01-12 Published:2022-01-13
  • Contact: Shufan Yin


: In this study, a novel series of cordycepin derivatives with benzenesulfonamido groups at the 6-position of the purine ring were synthesized and their antitumor activity was evaluated. We revealed the structural moieties of the cordycepin analogs that were required for antitumor activity. Among all the target compounds, those with 4-methyl and 4-nitro substituents on the benzene ring displayed better activity than the lead compound in antiproliferative activity experiments using MDA-MB-231 and A549 cells. However, compounds with 4-methoxybenzene and 2-oxoindoline groups and ethylene spacers displayed more significant activity than the lead compound in antiproliferative activity experiments using HeLa cells. In particular, a compound with a 4-bromo substituent and an ethylene spacer displayed very high inhibitory activity against the proliferation of MDA-MB-231, A549, and HeLa cells, suggesting that it had the potential for further development and application.

Key words: Cordycepin, Derivatives, Synthesis, Biological activity research