藤黄酚类似物的合成与生物学评价

Synthesis and biological evaluation of gambierol analogues.

作者信息

Fuwa Haruhiko, Kainuma Noriko, Satake Masayuki, Sasaki Makoto

机构信息

Graduate School of Science, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.

出版信息

Bioorg Med Chem Lett. 2003 Aug 4;13(15):2519-22. doi: 10.1016/s0960-894x(03)00467-0.

DOI:10.1016/s0960-894x(03)00467-0

PMID:12852956

Abstract

Gambierol is a polycyclic ether toxin, isolated as a toxic constituent from the marine dinoflagellate Gambierdiscus toxicus. We describe here the synthesis and biological evaluation of structural analogues of gambierol. The present preliminary structure-activity relationship studies clearly indicate that the H ring functionality and the unsaturated side chain of gambierol are crucial for its potent toxicity.

摘要

冈比毒素是一种多环醚毒素，从海洋甲藻剧毒冈比甲藻中分离出来作为一种有毒成分。我们在此描述冈比毒素结构类似物的合成及生物学评价。目前初步的构效关系研究清楚地表明，冈比毒素的H环官能团和不饱和侧链对其强毒性至关重要。