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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Detalles Bibliográficos
Autores principales: Chang, Jun, Hao, Yun-Peng, Hao, Xiao-Dong, Lu, Hong-Fu, Yu, Jian-Ming, Sun, Xun
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2013
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270178/
https://www.ncbi.nlm.nih.gov/pubmed/23973993
http://dx.doi.org/10.3390/molecules180910189
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author Chang, Jun
Hao, Yun-Peng
Hao, Xiao-Dong
Lu, Hong-Fu
Yu, Jian-Ming
Sun, Xun
author_facet Chang, Jun
Hao, Yun-Peng
Hao, Xiao-Dong
Lu, Hong-Fu
Yu, Jian-Ming
Sun, Xun
author_sort Chang, Jun
collection PubMed
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 pubmed-62701782018-12-18 Synthesis and Anti-HBV Activity of Novel 3′-N-phenylsulfonyl Docetaxel Analogs Chang, Jun Hao, Yun-Peng Hao, Xiao-Dong Lu, Hong-Fu Yu, Jian-Ming Sun, Xun Molecules Article 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. MDPI 2013-08-22 /pmc/articles/PMC6270178/ /pubmed/23973993 http://dx.doi.org/10.3390/molecules180910189 Text en © 2013 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Chang, Jun
Hao, Yun-Peng
Hao, Xiao-Dong
Lu, Hong-Fu
Yu, Jian-Ming
Sun, Xun
Synthesis and Anti-HBV Activity of Novel 3′-N-phenylsulfonyl Docetaxel Analogs
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 Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270178/
https://www.ncbi.nlm.nih.gov/pubmed/23973993
http://dx.doi.org/10.3390/molecules180910189
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