title: Synthesis and biological evaluation of novel beta-carboline derivatives as Tat-TAR interaction inhibitors.
abstract: 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.
authors.affiliation: National Research Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100083, China.
authors.forename: Xiaolin
authors.initials: X
authors.lastname: Yu
authors.forename: Wei
authors.initials: W
authors.lastname: Lin
authors.forename: Jingyun
authors.initials: J
authors.lastname: Li
authors.forename: Ming
authors.initials: M
authors.lastname: Yang
mesh_terms: 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
chemical_list: D019380:Anti-HIV Agents; D002243:Carbolines; D015696:Gene Products, tat