| Literature DB >> 16737818 |
Kenneth W Stagliano1, Ashkan Emadi, Zhenhai Lu, Helena C Malinakova, Barry Twenter, Min Yu, Louis E Holland, Amanda M Rom, John S Harwood, Ronak Amin, Allison A Johnson, Yves Pommier.
Abstract
Unsymmetrical biquinone and trimeric quinone derivatives were synthesized using halotriflate-biselectrophilic naphthoquinones through stepwise regioselective quinone substitution chemistry and evaluated for their ability to inhibit the cytopathogenic effects of HIV-1 using an MTT colorimetric assay. Compounds were also screened for their ability to inhibit the activity of HIV-1 integrase in vitro. Pyranylated trimeric quinones and biquinones exhibited both antiviral activity and integrase inhibitory activity. Conocurvone 1 and trimeric quinone 21 were the most potent HIV integrase inhibitors in the series. All of the biquinones showed HIV inhibitory activity. Simple methoxy substituted biquinones did not inhibit HIV-1 integrase.Entities:
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Year: 2006 PMID： 16737818 DOI： 10.1016/j.bmc.2006.04.034
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641