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J Med Chem. 2007 Jul 26;50(15):3416-9. Epub 2007 Jul 4.

Rationally designed dual inhibitors of HIV reverse transcriptase and integrase.

Abstract

Bifunctional inhibitors were designed and synthesized based on 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT)a1 non-nucleoside reverse transcriptase (RT) inhibitors and diketoacid (DKA) integrase (IN) inhibitors. Biochemical studies revealed activity against RT and IN at low nanomolar and low micromolar concentrations, respectively. Exceptionally low IC50 values from a cell-based assay were achieved along with remarkably high therapeutic indices. Compound 7 was identified as the best compound of the series (IC50: 24 nM against RT, 4.4 microM against IN, and 10 nM against HIV-1).

PMID:
17608468
DOI:
10.1021/jm070512p
[Indexed for MEDLINE]

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