Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1α inhibitors

被引：11

作者：

Huang, Wenwei ^{[1
]}

Huang, Ruili ^{[1
]}

Attene-Ramos, Matias S. ^{[1
]}

Sakamuru, Srilatha ^{[1
]}

Englund, Erika E. ^{[1
]}

Inglese, James ^{[1
]}

Austin, Christopher P. ^{[1
]}

Xia, Menghang ^{[1
]}

机构：

[1] NHGRI, NIH Chem Genom Ctr, NIH, Rockville, MD 20850 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 18期

基金：

美国国家卫生研究院;

关键词：

Hypoxia-inducible factor-1 alpha; Quinazolin-4-ones; Parallel synthesis; TARGETING HYPOXIA; HIF-1-ALPHA; IDENTIFICATION; ANGIOGENESIS; DERIVATIVES;

D O I：

10.1016/j.bmcl.2011.07.043

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Quinazolin-4-one 1 was identified as an inhibitor of the HIF-1 alpha transcriptional factor from a high-throughput screen. HIF-1 alpha up-regulation is common in many cancer cells. In this Letter, we describe an efficient one-pot sequential reaction for the synthesis of quinazolin-4-one 1 analogues. The structure-activity relationship (SAR) study led to the 5-fold more potent analogue, 16. Published by Elsevier Ltd.

引用

页码：5239 / 5243

页数：5

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