Synthesis and biological evaluation of Matijing-Su derivatives as potential anti-hepatitis B virus agents

作     者：Jing-Ying Qiu~1,Chang-Xiao Liu~2,Zheng-Ming Huang~3,Pei-Xue Cao~1,Wei-Dong Pan~1,Bi-Xue Xu~1,Xiao-Jiang Hao~1 and Guang-Yi Liang~(1,4,*) 1 The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences,202 Shachong South Road,Guiyang 550002,China 2 Tianjin Institute of Pharmaceutical Research,308 Anshan Xi Dao,Nankai District,Tianjin 300193,China 3 302 Hospital of PLA,100 Xisihuan Zhong Road,Fengtai Beijing 100039,China 4 Guiyang College of Traditional Chinese Medicine,50 Shidong Road,Guiyang 550002,China 

会议名称：《中药与天然药高峰论坛暨第十二届全国中药和天然药物学术研讨会》

会议日期：2012年

学科分类：1004[医学-公共卫生与预防医学(可授医学、理学学位)] 100401[医学-流行病与卫生统计学] 10[医学] 

关 键 词：MTS derivatives synthesis biological evaluation anti-hepatitis B virus activity 

摘      要：A series of Matijing-Su(MTS,N-(N-benzoyl-L-phenylalanyl)-O-acetyl-L -phenylalanol)derivatives were synthesized and evaluated for their abilities to inhibit the replication of hepatitis B virus(HBV)DNA in HepG2 2.2.15 *** 5r(IC:1.31 uM,SI:326.31),5f(IC:6.64 uM,SI:61.72),5a(IC:6.87 uM,SI:42.74),5d(IC:8.24 uM,SI:58.68)and 5h(IC:10.28 uM,SI:47.21)*** significant inhibitory on the replication of HBV DNA in 2.2.15 cells,which were better than those of the positive control lamivudine(IC:82.42 uM,SI:41.59).