Tryptamine derivatives as novel non-nucleosidic inhibitors against hepatitis B virus

  • Bioorg Med Chem. 2011 May 15;19(10):3120-7. doi: 10.1016/j.bmc.2011.04.004.
Shi-Jin Qu  1 ,  Gui-Feng Wang ,  Wen-Hu Duan ,  Shan-Yan Yao ,  Jian-Ping Zuo ,  Chang-Heng Tan ,  Da-Yuan Zhu
Affiliations
  • 1. Department of Natural Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
PMID: 21524588 DOI: 10.1016/j.bmc.2011.04.004
Abstract

A series of tryptamine derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. The preliminary SAR was discussed. Compounds 2e and 4a showed potent Antiviral activity (IC(50)=0.4 and <1 μM, respectively) and low cytotoxicity (CC(50)=40.6 and >25 μM, respectively).