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Elsevier, Bioorganic and Medicinal Chemistry Letters, 10(21), p. 2986-2990

DOI: 10.1016/j.bmcl.2011.03.047

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Development of Tricyclic Hydroxy-1H-pyrrolopyridine-trione Containing HIV-1 Integrase Inhibitors

Journal article published in 2011 by Xue Zhi Zhao ORCID, Kasthuraiah Maddali, Mathieu Metifiot, Steven J. Smith, B. Christie Vu, B. Christie Vu, Christophe Marchand, Stephen H. Hughes, Yves Pommier, Terrence R. Burke
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This paper is available in a repository.

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Abstract

New tricyclic HIV-1 integrase (IN) inhibitors were prepared that combined structural features of bicyclic pyrimidinones with recently disclosed 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones. This combination resulted in the introduction of a nitrogen into the aryl ring and the addition of a fused third ring to our previously described inhibitors. The resulting analogues showed low micromolar inhibitory potency in in vitro HIV-1 integrase assays, with good selectivity for strand transfer relative to 3′-processing.