伊曲拉米德B的全合成研究及其结构类似物的生物学评价。

Studies toward the total synthesis of Itralamide B and biological evaluation of its structural analogs.

作者信息

Wang Xiaoji, Lv Chanshan, Feng Junmin, Tang Linjun, Wang Zhuo, Liu Yuqing, Meng Yi, Ye Tao, Xu Zhengshuang

机构信息

School of Pharmacy, Jiangxi Science and Technology Normal University, Nanchang 330013, China.

Laboratory of Chemical Genomics, Peking University Shenzhen Graduate School, University Town of Shenzhen, Xili, Nanshan District, Shenzhen 518055, China.

出版信息

Mar Drugs. 2015 Apr 13;13(4):2085-104. doi: 10.3390/md13042085.

DOI:10.3390/md13042085

PMID:25871289

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4413201/

Abstract

Itralamides A and B were isolated from the lipophilic extract of Lyngbya majuscula collected from the eastern Caribbean. Itralamide B (1) showed cytotoxic activity towards human embryonic kidney cells (HEK293, IC50 = 6 μM). Preliminary studies disapproved the proposed stereochemistry of itralamide. In this paper, we will provide a full account of the total synthesis of four stereoisomers of itralamide B and the results derived from biological tests of these structural congeners.

摘要

从加勒比海东部采集的巨大鞘丝藻的亲脂性提取物中分离出了伊曲拉酰胺A和B。伊曲拉酰胺B（1）对人胚肾细胞（HEK293，IC50 = 6 μM）显示出细胞毒性活性。初步研究不支持伊曲拉酰胺提出的立体化学结构。在本文中，我们将全面阐述伊曲拉酰胺B的四种立体异构体的全合成以及这些结构类似物的生物学测试结果。