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Molecules 2013, 18(9), 10189-10212; doi:10.3390/molecules180910189

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

Department of Natural Products Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China
Author to whom correspondence should be addressed.
Received: 13 June 2013 / Revised: 15 August 2013 / Accepted: 17 August 2013 / Published: 22 August 2013
(This article belongs to the Section Medicinal Chemistry)
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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.
Keywords: 3′-N-phenylsulfonyl; docetaxel analogs; synthesis; anti-HBV 3′-N-phenylsulfonyl; docetaxel analogs; synthesis; anti-HBV

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Chang, J.; Hao, Y.-P.; Hao, X.-D.; Lu, H.-F.; Yu, J.-M.; Sun, X. Synthesis and Anti-HBV Activity of Novel 3′-N-phenylsulfonyl Docetaxel Analogs. Molecules 2013, 18, 10189-10212.

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