Synthesis and evaluation of beta-carboline derivatives as inhibitors of human immunodeficiency virus.
A series of beta-carboline derivatives were synthesized by utilizing aromatization and chemoselective alkylation method recently reported from our laboratory. Synthesized derivatives were evaluated for anti-HIV activity in human CD4+ T cell line (CEM-GFP) infected with HIV-1 NL(4.3) virus. 1-Formyl-beta-carboline-3-carbxylic acid methyl ester (15) showed inhibition of human immunodeficiency virus at IC(50)=2.9 microM.
Brahmbhatt
Keyur G
KG
Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), Punjab, India.
Ahmed
Nafees
N
Sabde
Sudeep
S
Mitra
Debashis
D
Singh
Inder Pal
IP
Bhutani
Kamlesh K
KK
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002243:Carbolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D005561:Formates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006678:HIV / Q000187:drug effects*; D006801:Humans
C553254:1-formyl-beta-carboline-3-carbxylic acid methyl ester; D019380:Anti-HIV Agents; D002243:Carbolines; D005561:Formates