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番荔枝科乙酰精宁的药物化学:新型类似物的设计、合成及生物学评价

Medicinal chemistry of Annonaceous acetogenins: design, synthesis, and biological evaluation of novel analogues.

作者信息

Kojima Naoto, Tanaka Tetsuaki

机构信息

Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamadaoka, Suita, Osaka, Japan.

出版信息

Molecules. 2009 Sep 17;14(9):3621-61. doi: 10.3390/molecules14093621.

DOI:10.3390/molecules14093621
PMID:19783948
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6254973/
Abstract

Most Annonaceous acetogenins are characterized by between one and three THF ring(s) with one or two flanking hydroxyl group(s) in the center of a C32/34 fatty acid, and the terminal carboxylic acid is combined with a 2-propanol unit to form an alpha,beta-unsaturated gamma-lactone. While many studies have addressed the properties and synthesis of natural acetogenins due to their attractive biological activities and unique structural features, a number of analogues have also been described. This review covers the design, synthesis, and biological evaluation of acetogenin analogues.

摘要

大多数番荔枝科杀精素的特征是在C32/34脂肪酸的中心有1至3个四氢呋喃环,环上带有1或2个位于侧翼的羟基,且末端羧酸与一个2-丙醇单元结合形成α,β-不饱和γ-内酯。由于天然杀精素具有吸引人的生物活性和独特的结构特征,许多研究都涉及了它们的性质和合成,同时也描述了一些类似物。这篇综述涵盖了杀精素类似物的设计、合成及生物学评价。

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