Chai Huifang, Zhao Yanfang, Zhao Chunshen, Gong Ping
School of Pharmceutical Engineering, Shenyang Pharmceutical University, PR China.
Bioorg Med Chem. 2006 Feb 15;14(4):911-7. doi: 10.1016/j.bmc.2005.08.041. Epub 2005 Sep 23.
A series of ethyl 6-bromo-5-hydroxy-1H-indole-3-carboxylates, 8a-11v, were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities in 2.2.15 cells. The selective indexes of inhibition on replication of HBV DNA of compounds 11s (>8.7) and 11t (10.8), which were introduced halogen on the phenyl ring at position 2, were greater than those of the other evaluated compounds including lamivudine (7.0). Compounds 9e, 9h, 9l, and 11v exhibited significant anti-HBV activities, and the IC(50) values on replication of HBV DNA of these compounds were 3.6, 6.37, 5.2, and 5.4 microg/ml, respectively, which were far more potent than the positive control lamivudine 228 microg/ml.
合成了一系列6-溴-5-羟基-1H-吲哚-3-羧酸乙酯（8a - 11v），并在2.2.15细胞中评估了它们的抗乙型肝炎病毒（HBV）活性。在2位苯环上引入卤素的化合物11s（>8.7）和11t（10.8）对HBV DNA复制的抑制选择性指数大于包括拉米夫定（7.）在内的其他评估化合物。化合物9e、9h、9l和11v表现出显著的抗HBV活性，这些化合物对HBV DNA复制的IC50值分别为3.6、6.37、5.2和5.4μg/ml，远比阳性对照拉米夫定的228μg/ml有效。
