2. Academic Validation
  3. Development of tricyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors

Development of tricyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors

  • Bioorg Med Chem Lett. 2011 May 15;21(10):2986-90. doi: 10.1016/j.bmcl.2011.03.047.
Xue Zhi Zhao 1,  Kasthuraiah Maddali,  Mathieu Metifiot,  Steven J Smith,  B Christie Vu,  Christophe Marchand,  Stephen H Hughes,  Yves Pommier,  Terrence R Burke Jr
Affiliations

Affiliation

  • 1 Chemical Biology Laboratory, Molecular Discovery Program, Center for Cancer Research, National Cancer Institute-Frederick, National Institutes of Health, Frederick, MD 21702, USA. xuezhi.zhao@nih.gov
PMID: 21493066 DOI: 10.1016/j.bmcl.2011.03.047
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.

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