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 activit...

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Veröffentlicht in:	Molecules (Basel, Switzerland) Switzerland), 2013-08, Vol.18 (9), p.10189-10212
Hauptverfasser:	Chang, Jun, Hao, Yun-Peng, Hao, Xiao-Dong, Lu, Hong-Fu, Yu, Jian-Ming, Sun, Xun
Format:	Artikel
Sprache:	eng
Schlagworte:	3′-N-phenylsulfonyl anti-HBV Antiviral Agents - chemical synthesis Antiviral Agents - pharmacology Cancer Docetaxel docetaxel analogs Drug Evaluation, Preclinical Hep G2 Cells Hepatitis B Hepatitis B virus - drug effects Humans Natural products Paclitaxel - pharmacology Structure-Activity Relationship Sulfones - chemical synthesis Sulfones - pharmacology synthesis Taxoids - chemical synthesis Taxoids - pharmacology
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Beschreibung
Zusammenfassung:	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 1420-3049
DOI:	10.3390/molecules180910189