Synthesis and Anti-HBV Activity of Novel 3′-N-phenylsulfonyl Docetaxel Analogs

Molecules

Jun Chang¹  Yun-Peng Hao¹  Xiao-Dong Hao¹  Hong-Fu Lu¹  Jian-Ming Yu¹ 

[1] id="af1-molecules-18-10189">Department of Natural Products Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, Chi

关键词: 3′-N-phenylsulfonyl;    docetaxel analogs;    synthesis;    anti-HBV;   

DOI  :  10.3390/molecules180910189

来源: mdpi

【 摘 要 】

Nine new 3′-N-phenylsulfonyl docetaxel analogs were synthesized in good yields from the key intermediate N-phenylsulfonyl oxazolidine via a six-step route. These analogs were tested for anti-hepatitis B virus (HBV) activity in vitro. Compounds 3e, 3g and 3j showed more potent inhibitory activity against HBeAg secretion than the positive control lamivudine. Further extensive SAR and mechanistic studies will be reported in due course.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.