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马蹄金素衍生物的合成及其抗乙型肝炎病毒活性研究(英文)

Synthesis and anti-hepatitis B virus activities of Matijing-Su derivatives

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【作者】 徐必学黄正明

【Author】 Bixue Xu~a,Zhengming Huang~b,Changxiao Liu~c,Zegui Cai~a,Weidong Pan~a, Peixue Cao~a,Xiaojiang Haoa and Guangyi Liang~a a The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences,202 Shachong South Road,Guiyang 550002,PR China b 302 Hospital of PLA,100 Xisihuan Zhong Road,Fengtai,Beijing 100039,PR China c Tianjin Institute of Pharmaceutical Research,308 Anshan Xi Dao,Nankai District,Tianjin 300193, PR China

【机构】 The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences 202 Shachong South Road,Guiyang 550002,PR China302 Hospital of PLA 100 Xisihuan Zhong Road,Fengtai,Beijing 100039,PR China

【摘要】 <正>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.

【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.

  • 【会议录名称】 第三届贵州省自然科学优秀学术论文评选获奖论文集(2010年)
  • 【会议时间】2010-06-01
  • 【分类号】R284.1;R285
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