马替净 - 苏衍生物的合成及其抗乙型肝炎病毒活性
Synthesis and anti-hepatitis B virus activities of Matijing-Su derivatives.
作者信息
Xu Bixue, Huang Zhengming, Liu Changxiao, Cai Zegui, Pan Weidong, Cao Peixue, Hao Xiaojiang, Liang Guangyi
机构信息
The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, 202 Shachong South Road, Guiyang 550002, PR China.
出版信息
Bioorg Med Chem. 2009 Apr 15;17(8):3118-25. doi: 10.1016/j.bmc.2009.03.003. Epub 2009 Mar 9.
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.
合成了一系列马替净素（MTS，N-（N-苯甲酰基-L-苯丙氨酰基）-O-乙酰基-L-苯丙醇）衍生物，并在2.2.15细胞中评估了它们的抗乙型肝炎病毒（HBV）活性。化合物9c（1.40微摩尔）、9g（2.33微摩尔）和9n（2.36微摩尔）等的半数抑制浓度（IC50）以及9n对HBV DNA复制抑制的选择性指数（45.93）高于阳性对照拉米夫定[41.59，（IC50：82.42微摩尔）]。化合物11d、12a和12e也表现出显著的抗HBV活性。
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