Rationally designed dual inhibitors of HIV reverse transcriptase and integrase

Research output: Contribution to journalArticlepeer-review

78 Scopus citations

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 μM against IN, and 10 nM against HIV-1).

Original languageEnglish (US)
Pages (from-to)3416-3419
Number of pages4
JournalJournal of medicinal chemistry
Volume50
Issue number15
DOIs
StatePublished - Jul 26 2007

Fingerprint Dive into the research topics of 'Rationally designed dual inhibitors of HIV reverse transcriptase and integrase'. Together they form a unique fingerprint.

Cite this