In vitro anti-human immunodeficiency virus (HIV) activity of the chromanone derivative, 12-oxocalanolide A, a novel NNRTI

The three chromanone derivatives, (+)-, (−)-, and (±)-12-oxocalanolide A ( 2), were evaluated for in vitro antiviral activities against HIV and simian immunodeficiency virus (SIV). The compounds were determined to be inhibitors of HIV-1 reverse transcriptase (RT) and exhibited activity against a var...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 1998-08, Vol.8 (16), p.2179-2184
Hauptverfasser: Ze-Qi Xu, Buckheit, Robert W., Stup, Tracy L., Flavin, Michael T., Khilevich, Albert, Rizzo, John D., Lin, Lin, Zembower, David E.
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Sprache:eng
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Zusammenfassung:The three chromanone derivatives, (+)-, (−)-, and (±)-12-oxocalanolide A ( 2), were evaluated for in vitro antiviral activities against HIV and simian immunodeficiency virus (SIV). The compounds were determined to be inhibitors of HIV-1 reverse transcriptase (RT) and exhibited activity against a variety of viruses selected for resistance to other HIV-1 nonnucleoside RT inhibitors. They are the first reported calanolide analogues capable of inhibiting SIV. The three chromanone derivatives, (+)-, (−)-, and (±)-12-oxocalanolide A ( 2), were evaluated for in vitro antiviral activities against HIV and SIV. The compounds were determined to be inhibitors of HIV-1 reverse transcriptase (RT) and exhibited activity against a variety of viruses selected for resistance to other HIV-1 nonnucleoside RT inhibitors. They are the first reported calanolide analogues capable of inhibiting SIV.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(98)00380-1