Syntheses and antiproliferative evaluation of oxyphenisatin derivatives

The syntheses and structure–antiproliferative relationship for oxyphenisatin analogues are reported. Syntheses and structure–antiproliferative relationship for oxyphenisatin analogues are described. The cell proliferation data showed that the presence of substituents (especially F, Cl, Me, CF 3, and...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2007-05, Vol.17 (10), p.2854-2857
Hauptverfasser: Uddin, Muhammed K., Reignier, Serge G., Coulter, Tom, Montalbetti, Christian, Grånäs, Charlotta, Butcher, Steven, Krog-Jensen, Christian, Felding, Jakob
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Sprache:eng
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Zusammenfassung:The syntheses and structure–antiproliferative relationship for oxyphenisatin analogues are reported. Syntheses and structure–antiproliferative relationship for oxyphenisatin analogues are described. The cell proliferation data showed that the presence of substituents (especially F, Cl, Me, CF 3, and OMe) in the 6- and 7-position of oxyphenisatin markedly enhanced the potency in the MDA-468 cell line without affecting the MDA-231 cell line. The best compounds from this series showed low nanomolar antiproliferative activity towards the MDA-468 cell line and a 1000-fold selectivity over the MDA-231 cell line.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.02.060