Longeon A., Copp B. R., Roué M., Dubois J., Valentin A., Petek Sylvain, Debitus Cécile, Bourguet-Kondracki M. L. (2010). New bioactive halenaquinone derivatives from South Pacific marine sponges of the genus Xestospongia. Bioorganic and Medicinal Chemistry, 18 (16), p. 6006-6011. ISSN 0968-0896.
Titre du document
New bioactive halenaquinone derivatives from South Pacific marine sponges of the genus Xestospongia
Longeon A., Copp B. R., Roué M., Dubois J., Valentin A., Petek Sylvain, Debitus Cécile, Bourguet-Kondracki M. L.
Source
Bioorganic and Medicinal Chemistry, 2010,
18 (16), p. 6006-6011 ISSN 0968-0896
Bioassay-directed fractionation of South Pacific marine sponges of the genus Xestospongia has led to the isolation of a number of halenaquinone-type polyketides, including two new derivatives named xestosaprol C methylacetal 7 and orhalquinone 8. Chemical characterization of these two new compounds was achieved by extensive 1D and 2D NMR spectroscopic studies. Evaluation of anti-phospholipase A(2), anti-farnesyltransferase and antiplasmodial activities of this series is presented and structure/activity relationships are discussed. Orhalquinone 8 displayed a significant inhibition of both human and yeast farnesyltransferase enzymes, with IC50 value of 0.40 mu M and was a moderate growth inhibitor of Plasmodium falciparum.
