源自鼠尾草的咖啡酸二聚体的合成及其对HIV-1整合酶的抑制活性
Synthesis and HIV-1 integrase inhibitory activities of caffeic acid dimers derived from Salvia officinalis.
作者信息
Bailly Fabrice, Queffelec Clémence, Mbemba Gladys, Mouscadet Jean-François, Cotelle Philippe
机构信息
Laboratoire de Chimie Organique et Macromoléculaire, UMR CNRS 8009, Université des Sciences et Technologies de Lille I, 59655 Villeneuve d'Ascq, France.
出版信息
Bioorg Med Chem Lett. 2005 Nov 15;15(22):5053-6. doi: 10.1016/j.bmcl.2005.07.091. Epub 2005 Sep 23.
The synthesis of two caffeoyl-coumarin conjugates, derived from sagecoumarin, has been accomplished, starting from ferulic acid, isoferulic acid and sesamol. Both compounds exhibited potent inhibitory activities at micromolar concentrations against HIV-1 integrase in 3'-end processing reaction but were less effective against HIV-1 replication in a single-round infection assay of HeLa-beta-gal-CD4+ cells.
以阿魏酸、异阿魏酸和芝麻酚为原料，完成了两种源自鼠尾草香豆素的咖啡酰香豆素共轭物的合成。在3'-末端加工反应中，两种化合物在微摩尔浓度下均对HIV-1整合酶表现出强效抑制活性，但在HeLa-β-半乳糖苷酶-CD4+细胞的单轮感染试验中，它们对HIV-1复制的抑制效果较差。
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