Department of Natural Products Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China.
Molecules. 2013 Aug 22;18(9):10189-212. doi: 10.3390/molecules180910189.
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.
从关键中间体 N-苯磺酰基恶唑烷通过六步反应路线，以良好的收率合成了 9 种新型 3'-N-苯磺酰基多西他赛类似物。这些类似物在体外进行了抗乙型肝炎病毒（HBV）活性测试。化合物 3e、3g 和 3j 对 HBeAg 分泌的抑制活性强于阳性对照拉米夫定。进一步的广泛 SAR 和机制研究将在适当的时候报告。
