Identification of a dibenzocyclooctadiene lignan as a HIV-1 non-nucleoside reverse transcriptase inhibitor.
Antivir Chem Chemother
; 24(1): 28-38, 2015 Feb.
Article
em En
| MEDLINE
| ID: mdl-26149264
ABSTRACT
BACKGROUND:
Due to resistance to all classes of anti-HIV drugs and drug toxicity, there is a need for the discovery and development of new anti-HIV drugs.METHODS:
HIV-1 inhibitors were identified and biologically characterized for mechanism of action.RESULTS:
We identified a dibenzocyclooctadiene lignan, termed HDS2 that possessed anti-HIV activity against a wide variety of viral strains with EC50 values in the 1-3 µM range. HDS2 was shown to act as an NNRTI by qPCR and in vitro enzyme assays.CONCLUSIONS:
This compound provides a new scaffold for further optimization of activity through structure-guided design.Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
HIV-1
/
Lignanas
/
Inibidores da Transcriptase Reversa
/
Ciclo-Octanos
/
Transcriptase Reversa do HIV
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article