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Elsevier, Bioorganic and Medicinal Chemistry Letters, 10(19), p. 2714-2717

DOI: 10.1016/j.bmcl.2009.03.122

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Examination of halogen substituent effects on HIV-1 integrase inhibitors derived from 2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-ones and 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones

Journal article published in 2009 by Xue Zhi Zhao ORCID, Kasthuraiah Maddali, 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

Using 2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-one and 4,5-dihydroxy-1H-isoindole-1,3(2H)-dione based HIV-1 integrase inhibitors as display platforms, we undertook a thorough examination of the effects of modifying the halogen substituents on a key benzyl ring that is hypothesized to bind in a hydrophobic pocket of the integrase•DNA complex. Data from this study suggest that in general dihalo – substituted analogues have higher potency than monohalo – substituted compounds, but that further addition of halogens is not beneficial.