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New bioactive halenaquinone derivatives from South Pacific marine sponges of the genus Xestospongia.

机译:Xestospongia属的南太平洋海洋海绵中的新生物活性卤代醌衍生物。

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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 IC(50) value of 0.40 microM and was a moderate growth inhibitor of Plasmodium falciparum.
机译:生物测定法指导的南太平洋海藻海绵的分离已导致分离出多种卤代对苯二酚型聚酮化合物,包括名为xestosaprol C甲基缩醛7和邻苯二酚8的两种新衍生物。这两种新化合物的化学表征通过广泛的1D和2D NMR光谱研究。评价了该系列的抗磷脂酶A(2),抗法呢基转移酶和抗血浆活性,并讨论了结构/活性关系。 Orhalquinone 8表现出对人和酵母法呢基转移酶的显着抑制,IC(50)值为0.40 microM,是恶性疟原虫的中度生长抑制剂。

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