title: Tryptamine derivatives as novel non-nucleosidic inhibitors against hepatitis B virus.
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).
authors.affiliation: Department of Natural Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
authors.forename: Shi-Jin
authors.initials: SJ
authors.lastname: Qu
authors.forename: Gui-Feng
authors.initials: GF
authors.lastname: Wang
authors.forename: Wen-Hu
authors.initials: WH
authors.lastname: Duan
authors.forename: Shan-Yan
authors.initials: SY
authors.lastname: Yao
authors.forename: Jian-Ping
authors.initials: JP
authors.lastname: Zuo
authors.forename: Chang-Heng
authors.initials: CH
authors.lastname: Tan
authors.forename: Da-Yuan
authors.initials: DY
authors.lastname: Zhu
mesh_terms: D000998:Antiviral Agents / Q000737:chemistry* / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D004279:DNA, Viral / Q000378:metabolism; D056945:Hep G2 Cells; D006509:Hepatitis B / Q000188:drug therapy*; D006515:Hepatitis B virus / Q000187:drug effects*; D006801:Humans; D013329:Structure-Activity Relationship; D014363:Tryptamines / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000998:Antiviral Agents; D004279:DNA, Viral; D014363:Tryptamines; C030820:tryptamine