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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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:
Online Access:http://www.mdpi.com/1420-3049/18/9/10189
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author Xun Sun
Jian-Ming Yu
Hong-Fu Lu
Xiao-Dong Hao
Yun-Peng Hao
Jun Chang
author_facet Xun Sun
Jian-Ming Yu
Hong-Fu Lu
Xiao-Dong Hao
Yun-Peng Hao
Jun Chang
author_sort Xun Sun
collection DOAJ
description 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.
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spelling doaj.art-113ccf9e87614101b17461b2f4f8242b2022-12-22T01:19:54ZengMDPI AGMolecules1420-30492013-08-01189101891021210.3390/molecules180910189Synthesis and Anti-HBV Activity of Novel 3′-N-phenylsulfonyl Docetaxel AnalogsXun SunJian-Ming YuHong-Fu LuXiao-Dong HaoYun-Peng HaoJun ChangNine 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.http://www.mdpi.com/1420-3049/18/9/101893′-N-phenylsulfonyldocetaxel analogssynthesisanti-HBV
spellingShingle Xun Sun
Jian-Ming Yu
Hong-Fu Lu
Xiao-Dong Hao
Yun-Peng Hao
Jun Chang
Synthesis and Anti-HBV Activity of Novel 3′-N-phenylsulfonyl Docetaxel Analogs
Molecules
3′-N-phenylsulfonyl
docetaxel analogs
synthesis
anti-HBV
title Synthesis and Anti-HBV Activity of Novel 3′-N-phenylsulfonyl Docetaxel Analogs
title_full Synthesis and Anti-HBV Activity of Novel 3′-N-phenylsulfonyl Docetaxel Analogs
title_fullStr Synthesis and Anti-HBV Activity of Novel 3′-N-phenylsulfonyl Docetaxel Analogs
title_full_unstemmed Synthesis and Anti-HBV Activity of Novel 3′-N-phenylsulfonyl Docetaxel Analogs
title_short Synthesis and Anti-HBV Activity of Novel 3′-N-phenylsulfonyl Docetaxel Analogs
title_sort synthesis and anti hbv activity of novel 3 n phenylsulfonyl docetaxel analogs
topic 3′-N-phenylsulfonyl
docetaxel analogs
synthesis
anti-HBV
url http://www.mdpi.com/1420-3049/18/9/10189
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