title: Synthesis of hemslecin A derivatives: a new class of hepatitis B virus inhibitors.
abstract: A series of hemslecin A derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities, namely, inhibiting the secretion of hepatitis B surface antigen (HBsAg), hepatitis B e antigen (HBeAg), and HBV DNA replication on HepG 2.2.15 cells. Most of the derivatives showed enhanced anti-HBV activities, of which compounds A1-A7, B5, C and E exhibited significant activities inhibiting HBV DNA replication with IC(50) values of 2.8-11.6 μM, comparable to that of the positive control, tenofovir. Compounds A1-A3, A5, B5, and C displayed low cytotoxicities, which resulted in high SI values of 89.7, 55.6, 77.8, >83.4, >55.8, and >150.5, respectively.
authors: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, PR China.
authors: Rui-Hua
authors: RH
authors: Guo
authors: Chang-An
authors: CA
authors: Geng
authors: Xiao-Yan
authors: XY
authors: Huang
authors: Yun-Bao
authors: YB
authors: Ma
authors: Quan
authors: Q
authors: Zhang
authors: Li-Jun
authors: LJ
authors: Wang
authors: Xue-Mei
authors: XM
authors: Zhang
authors: Rong-Ping
authors: RP
authors: Zhang
authors: Ji-Jun
authors: JJ
authors: Chen
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D019662:Cucurbitaceae / Q000737:chemistry; D054728:Cucurbitacins / Q000138:chemical synthesis* / Q000494:pharmacology*; D004279:DNA, Viral / Q000302:isolation & purification; D056945:Hep G2 Cells; D006515:Hepatitis B virus / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D004279:DNA, Viral; D054728:Cucurbitacins