Synthesis and biological evaluation of novel beta-carboline derivatives as Tat-TAR interaction inhibitors.
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.
Yu
Xiaolin
X
National Research Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100083, China.
Lin
Wei
W
Li
Jingyun
J
Yang
Ming
M
D019380:Anti-HIV Agents / Q000737:chemistry* / Q000494:pharmacology*; D002243:Carbolines / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D004353:Drug Evaluation, Preclinical / Q000379:methods; D015696:Gene Products, tat / Q000037:antagonists & inhibitors* / Q000378:metabolism; D016325:HIV Long Terminal Repeat / Q000187:drug effects* / Q000502:physiology; D006801:Humans
D019380:Anti-HIV Agents; D002243:Carbolines; D015696:Gene Products, tat