Synthesis and anti-HIV activity of novel 2',3'-dideoxy-3'-thiacytidine prodrugs.
Bioorg Med Chem
; 17(17): 6407-13, 2009 Sep 01.
Article
em En
| MEDLINE
| ID: mdl-19660957
ABSTRACT
We report here the synthesis of a novel series of 5'-O-carbonates of 3TC, using different aliphatic alcohols and N,N-carbonyldiimidazol. Its antiviral activity was determined in peripheral blood mononuclear cells (PBMCs) showing some carbonate derivatives with an activity similar to or better than 3TC, except 3TC-Metha and 3TC-2Pro with less activity. In vitro assays in PBMCs have demonstrated that cytotoxicity increases as the carbon chain length of the alcohol moiety increases, showing compounds with a normal chain length of n=2-5 good selective index, compared to the parent drug. Thus, this work is an important contribution leading to the suppression of HIV replication.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pró-Fármacos
/
Lamivudina
/
Fármacos Anti-HIV
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem
Ano de publicação:
2009
Tipo de documento:
Article