Total synthesis of Calebin-A, preparation of its analogues, and their neuronal cell protectivity against β-amyloid insult

被引：39

作者：

Kim, DSHL

Kim, JY

机构：

[1] Univ Illinois, Coll Pharm, Program Collaborat Res Pharmaceut Sci, Chicago, IL 60612 USA

[2] Univ Illinois, Coll Pharm, Dept Med Chem & Pharmacognosy, Chicago, IL 60612 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(01)00489-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A total synthesis of Calebin-A (1), a novel curcuminoid isolated from turmeric (Curcuma longa, Zingiberaceae) that has been demonstrated to protect neuronal cells from beta -amyloid insult, was successfully achieved in four steps. Elaborating on this synthetic route. 13 analogues were prepared for a structure-activity relationship (SAR) study. It was found that the parent compound 1 and derivatives 21, 28, and 30 protect PC12 rat pheocromocytoma and IMR-32 human neuroblastoma cells from beta -amyloid(25-35) insult. These results suggest that hydroxy group at para-position is most critical for the expression of biological activity. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2541 / 2543

页数：3

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