Analysis of HIF-1 inhibition by manassantin A and analogues with modified tetrahydrofuran configurations

被引：26

作者：

Kasper, Amanda C. ^{[1
]}

Moon, Eui Jung ^{[2
]}

Hu, Xiangqian ^{[1
]}

Park, Yongho ^{[1
]}

Wooten, Ceshea M. ^{[1
]}

Kim, Hyoungsu ^{[1
]}

Yang, Weitao ^{[1
]}

Dewhirst, Mark W. ^{[2
,3
]}

Hong, Jiyong ^{[1
]}

机构：

[1] Duke Univ, Dept Chem, Durham, NC 27708 USA

[2] Duke Univ, Dept Pathol, Med Ctr, Durham, NC 27708 USA

[3] Duke Univ, Med Ctr, Dept Radiat Oncol, Durham, NC 27708 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 14期

基金：

美国国家卫生研究院;

关键词：

Manassantin A; Hypoxia; Hypoxia inducible factor-1; Tetrahydrofuran analogue; Tetrahydrofuran configuration; Vascular endothelial growth factor; 2,3-cis-3,4-trans-4,5-cis-Tetrahydrofuran; 2,3-cis-3,4-trans-4,5-trans-Tetrahydrofuran; 2,3-trans-3,4-trans-4,5-trans-Tetrahydrofuran; Conformation-activity relationship; INDUCIBLE FACTOR-I; STEREOSELECTIVE-SYNTHESIS; HYPOXIA; FACTOR-1-ALPHA; ANGIOGENESIS; EXPRESSION; THERAPY; LIGNANS; CELLS; HEAD;

D O I：

10.1016/j.bmcl.2009.04.071

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have shown that manassantin A downregulated the HIF-1 alpha expression and inhibited the secretion of VEGF. We have also demonstrated that the 2,3-cis-3,4-trans-4,5-cis-configuration of the tetrahydrofuran is critical to the HIF-1 inhibition of manassantin A. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：3783 / 3786

页数：4

共 31 条

[1]

Aebersold DM, 2001, CANCER RES, V61, P2911

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