1,5-Benzodiazepines. Part XII. Synthesis and biological evaluation of tricyclic and tetracyclic 1,5-benzodiazepine derivatives as nevirapine analogues.
Eur J Med Chem
; 36(11-12): 935-49, 2001.
Article
en En
| MEDLINE
| ID: mdl-11755236
A number of properly substituted 5H-pyrimido[4,5-b][1,5]benzodiazepines (2) and pyrazolo[3,4-b][1,5]benzodiazepines (3 and 4), as well as compounds 5-7, which are derivatives of new tetracyclic systems, were prepared as nevirapine analogues through multistep synthetic routes. The cytotoxic and anti-HIV-1 properties of compounds 2-7 were evaluated in cell-based assays, together with their inhibitory activity against the HIV-1 recombinant reverse transcriptase (rRT) in enzyme assays. The modifications introduced into nevirapine heterocyclic skeleton proved to have a negative effect for the anti-HIV-1 activity. It is worth noting that some of the new derivatives proved to be cytotoxic in the low micromolar range.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Benzodiazepinas
/
Linfocitos T
/
VIH-1
/
Inhibidores de la Transcriptasa Inversa
/
Nevirapina
Límite:
Humans
Idioma:
En
Revista:
Eur J Med Chem
Año:
2001
Tipo del documento:
Article
País de afiliación:
Italia
Pais de publicación:
Francia