Design, synthesis and evaluation of novel 2H-1, 4-benzodiazepine-2-ones as inhibitors of HIV-1 transcription

Journal Article

HIV-1 trans-activator of transcription (Tat) plays a critical role in HIV-1 transcription. Based on the β-turn motif present in HIV-1 Tat, a series of novel benzodiazepine analogs were designed as β-turn mimetics and prepared from p-chloro-nitrobenzene/2-phenylacetonitrile, p-toluidine/benzoyl chloride, or (Z)-7-nitro-5-phenyl-1H-benzo[e][1, 4]diazepin-2(3H)-one (nitrazepam) through different synthetic routes. Preliminary biological evaluation indicated that compound 30 exhibited inhibitory activity on HIV-1 tat-mediated LTR transcription with EC50 of 25.0 μmol·L-1 and showed no obvious cytotoxic effects on TZM-B1 cells under the concentration of 100 μmol·L-1.

Duke Authors

Cited Authors

  • Tang, Y-B; Zhang, C-M; Fang, C; Hu, C; Huang, L; Chen, C-H; Xiao, Z-Y

Published Date

  • 2011

Published In

Volume / Issue

  • 46 / 6

Start / End Page

  • 688 - 694

PubMed ID

  • 21882530

International Standard Serial Number (ISSN)

  • 0513-4870