title: Synthesis and anti-HBV activity of novel 3'-N-phenylsulfonyl docetaxel analogs.
abstract: 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.
authors: Department of Natural Products Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China.
authors: Jun
authors: J
authors: Chang
authors: Yun-Peng
authors: YP
authors: Hao
authors: Xiao-Dong
authors: XD
authors: Hao
authors: Hong-Fu
authors: HF
authors: Lu
authors: Jian-Ming
authors: JM
authors: Yu
authors: Xun
authors: X
authors: Sun
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000077143:Docetaxel; D004353:Drug Evaluation, Preclinical; D056945:Hep G2 Cells; D006515:Hepatitis B virus / Q000187:drug effects*; D006801:Humans; D017239:Paclitaxel / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000138:chemical synthesis* / Q000494:pharmacology; D043823:Taxoids / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000998:Antiviral Agents; D013450:Sulfones; D043823:Taxoids; D000077143:Docetaxel; D017239:Paclitaxel
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