Bioorganic & medicinal chemistry letters

Synthesis and biological evaluation of novel β-carboline derivatives as Tat–TAR interaction inhibitors

X Yu, W Lin, J Li, M Yang

文献索引：Yu, Xiaolin; Lin, Wei; Li, Jingyun; Yang, Ming Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 12 p. 3127 - 3130

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被引用次数: 45

摘要

Four new β-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.