Design, synthesis and evaluation of novel 2H-1, 4-benzodiazepine-2-ones as inhibitors of HIV-1 transcription / 药学学报
Acta Pharmaceutica Sinica
;
(12): 688-694, 2011.
Artigo
em Chinês
| WPRIM
| ID: wpr-348899
ABSTRACT
HIV-1 trans-activator of transcription (Tat) plays a critical role in HIV-1 transcription. Based on the beta-turn motif present in HIV-1 Tat, a series of novel benzodiazepine analogs were designed as beta-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 micromol x L(-1) and showed no obvious cytotoxic effects on TZM-BI cells under the concentration of 100 micromol x L(-1).
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Transcrição Gênica
/
Benzodiazepinonas
/
Química
/
Repetição Terminal Longa de HIV
/
HIV-1
/
Linhagem Celular Tumoral
/
Produtos do Gene tat do Vírus da Imunodeficiência Humana
/
Genética
Limite:
Humanos
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2011
Tipo de documento:
Artigo
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