title: Synthesis and anti-hepatitis B virus activities of Matijing-Su derivatives.
abstract: A series of derivatives of Matijing-Su (MTS, N-(N-benzoyl-L-phenylalanyl)-O-acetyl-L-phenylalanol) was synthesized and evaluated for their anti-hepatitis B virus (HBV) activities in 2.2.15 cells. The IC(50) of compounds 9c (1.40 microM), 9g (2.33 microM) and 9n (2.36 microM), etc. and the selective index of 9n (45.93) of the inhibition on the replication of HBV DNA were higher than those of the positive control lamivudine [41.59, (IC(50): 82.42 microM)]. Compounds 11d, 12a and 12e also exhibited significant anti-HBV activities.
authors.affiliation: The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, 202 Shachong South Road, Guiyang 550002, PR China.
authors.forename: Bixue
authors.initials: B
authors.lastname: Xu
authors.forename: Zhengming
authors.initials: Z
authors.lastname: Huang
authors.forename: Changxiao
authors.initials: C
authors.lastname: Liu
authors.forename: Zegui
authors.initials: Z
authors.lastname: Cai
authors.forename: Weidong
authors.initials: W
authors.lastname: Pan
authors.forename: Peixue
authors.initials: P
authors.lastname: Cao
authors.forename: Xiaojiang
authors.initials: X
authors.lastname: Hao
authors.forename: Guangyi
authors.initials: G
authors.lastname: Liang
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D006515:Hepatitis B virus / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D020128:Inhibitory Concentration 50; D019259:Lamivudine / Q000494:pharmacology; D015394:Molecular Structure; D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D019259:Lamivudine; D010649:Phenylalanine