HIF-1α inhibitors: Synthesis and biological evaluation of novel moracin O and P analogues

被引：53

作者：

Xia, Yan ^{[1
]}

Jin, Yinglan ^{[1
]}

Kaur, Navneet ^{[1
]}

Choi, Yongseok ^{[2
]}

Lee, Kyeong ^{[1
]}

机构：

[1] Dongguk Univ Seoul, Coll Pharm, Seoul 100715, South Korea

[2] Korea Univ, Dept Life Sci & Biotechnol, Seoul 136701, South Korea

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 06期

关键词：

Moracin; Arylbenzofuran; HIF-1; alpha; Structure-activity relationships; INDUCIBLE FACTOR-I; HIF-1; PAS; IDENTIFICATION; FAMILY; TARGET; MODEL;

D O I：

10.1016/j.ejmech.2011.03.022

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The natural products moracins O and P exhibited potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1), which is a key mediator during adaptation of cancer cells to tumour hypoxia. Systematic variations of the structures of benzofuran type moracins were made and structure-activity relationship analysis showed the importance of the 2-arylbenzofuran ring and the (R)-configuration of the core scaffold. Further evaluation of the representative compound 5 showed its inhibitory effect on HIF-1 alpha protein accumulation and target gene expression under hypoxia. (C) 2011 Elsevier Masson SAS. All rights reserved.

引用

页码：2386 / 2396

页数：11

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