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维生素K2的ω-氧化类似物的高效合成及生物学评价:维生素K2代谢产物的修饰及构效关系研究

Efficient synthesis and biological evaluation of omega-oxygenated analogues of vitamin K2: study of modification and structure-activity relationship of vitamin K2 metabolites.

作者信息

Suhara Yoshitomo, Murakami Aya, Kamao Maya, Mimatsu Shino, Nakagawa Kimie, Tsugawa Naoko, Okano Toshio

机构信息

Department of Hygienic Sciences, Kobe Pharmaceutical University, 4-19-1 Motoyamakita-machi, Higashinada-ku, Kobe 658-8558, Japan.

出版信息

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1622-5. doi: 10.1016/j.bmcl.2006.12.082. Epub 2007 Jan 4.

Abstract

Novel omega-oxygenated vitamin K2 analogues, which are candidates for metabolites of vitamin K2 homologues, were efficiently synthesized and their apoptosis-inducing activity was evaluated. We revealed that some of those analogues were biologically active and the side-chain part played an important role in apoptosis-inducing activity. Our results can provide useful information to develop the structure-activity relationship of vitamin K2 analogues for new drugs based on vitamin K.

摘要

新型ω-氧化维生素K2类似物作为维生素K2同系物的代谢物候选物被高效合成,并对其诱导细胞凋亡的活性进行了评估。我们发现其中一些类似物具有生物活性,且侧链部分在诱导细胞凋亡活性中起重要作用。我们的结果可为基于维生素K开发新型药物的维生素K2类似物的构效关系研究提供有用信息。

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