Cytotoxic and Protein Kinase Inhibiting Nakijiquinones and Nakijiquinols from the Sponge Dactylospongia metachromia

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• 作者：Georgios Daletos ; Nicole J. de Voogd ; Werner E. G. M眉ller ; Victor Wray ; WenHan Lin ; Daniel Feger ; Michael Kubbutat ; Amal H. Aly ; Peter Proksch
• 刊名：Journal of Natural Products
• 出版年：2014
• 出版时间：February 28, 2014
• 年：2014
• 卷：77
• 期：2
• 页码：218-226
• 全文大小：342K
• 年卷期：v.77,no.2(February 28, 2014)
• ISSN：1520-6025

文摘

Chemical investigation of the sponge Dactylospongia metachromia afforded five new sesquiterpene aminoquinones (1鈥?b>5), two new sesquiterpene benzoxazoles (6 and 7), the known analogue 18-hydroxy-5-epi-hyrtiophenol (8), and a known glycerolipid. The structures of all compounds were unambiguously elucidated by one- and two-dimensional NMR and by MS analyses, as well as by comparison with the literature. Compounds 1鈥?b>5 showed potent cytotoxicity against the mouse lymphoma cell line L5178Y with IC₅₀ values ranging from 1.1 to 3.7 渭M. When tested in vitro for their inhibitory potential against 16 different protein kinases, compounds 5, 6, and 8 exhibited the strongest inhibitory activity against ALK, FAK, IGF1-R, SRC, VEGF-R2, Aurora-B, MET wt, and NEK6 kinases (IC₅₀ 0.97鈥?.62 渭M).