Yu Xiaolin, Lin Wei, Li Jingyun, Yang Ming
National Research Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100083, China.
Bioorg Med Chem Lett. 2004 Jun 21;14(12):3127-30. doi: 10.1016/j.bmcl.2004.04.022.
Four new beta-carboline derivatives were synthesized bearing guanidinium group or amino group-terminated side chain targeting the TAR element. Compounds 5 and 6 with terminal guanidinium group showed inhibitory activities on Tat-TAR interaction as well as to HIV-1 in MT4 cells. Furthermore, capillary electrophoresis assay implied that compound 6 could not only bind to TAR but also hinder the Tat-TAR interaction.
合成了四种带有胍基或氨基末端侧链的新型β-咔啉衍生物，其靶向TAR元件。带有末端胍基的化合物5和6对Tat-TAR相互作用以及MT4细胞中的HIV-1均表现出抑制活性。此外，毛细管电泳分析表明化合物6不仅可以与TAR结合，还能阻碍Tat-TAR相互作用。
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