Rationally designed dual inhibitors of HIV reverse transcriptase and integrase

Zhengqiang Wang, Eric M. Bennett, Daniel J. Wilson, Christine Salomon, Robert Vince

Research output: Contribution to journalArticlepeer-review

90 Scopus citations


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
Issue number15
StatePublished - Jul 26 2007


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