| Literature DB >> 21493066 |
Xue Zhi Zhao1, Kasthuraiah Maddali, Mathieu Metifiot, Steven J Smith, B Christie Vu, Christophe Marchand, Stephen H Hughes, Yves Pommier, Terrence R Burke.
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. Published by Elsevier Ltd.Entities:
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Year: 2011 PMID： 21493066 PMCID： PMC3085635 DOI： 10.1016/j.bmcl.2011.03.047
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823