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

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

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 aga...

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Bibliographic Details
Main Authors: Xun Sun, Jian-Ming Yu, Hong-Fu Lu, Xiao-Dong Hao, Yun-Peng Hao, Jun Chang
Format: Article
Language:English
Published: MDPI AG 2013-08-01
Series:Molecules
Subjects:
3′-N-phenylsulfonyl
docetaxel analogs
synthesis
anti-HBV
Online Access:http://www.mdpi.com/1420-3049/18/9/10189
Description
Summary: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.
ISSN:1420-3049

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