Citation: Ying Chen, Jin Zhou, Hai Wang, Yi Xia, Zheng Yu Yang, Peng Xia. Synthesis and anti-HBV activity of S-substituted 7-mercapto-4-methylcoumarin analogs[J]. Chinese Chemical Letters, ;2008, 19(8): 925-927. doi: 10.1016/j.cclet.2008.05.043 shu

Synthesis and anti-HBV activity of S-substituted 7-mercapto-4-methylcoumarin analogs

Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 200032, China

Received Date: 31 March 2008

Fund Project: This research was supported by a grant from National Science Foundation of China (No.20272010 and 30200348) awarded to P.Xia and Y.Chenrespectively

Twelve S-substituted 7-mercapto-4-methylcoumarin analogs were synthesized and evaluated for the inhibition to HBV in HepG2 2.2.1.5 cell.Among them, ten compounds exhibited potent inhibition to HBsAg and/or HBeAg with the IC₅₀ values of subμmol/L level.The IC₅₀ of anti-HBsAg activities of 5c and 5j reached 0.01 μmol/L respectively which were 16 fold more potent than that of 3TC.Compounds 3, 5e, 5g, 5h and 5i showed admirable inhibitory activity to both HBsAg and HBeAg.The bioassay results indicated the S-substituted 7-mercapto-4-methylcoumarin analogs merit attention as novel anti-HBV agents.
- Synthesis,
- S-Substituted 7-mercapto-4-methylcoumarin,
- Anti-HBV
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