Design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as STAT3 inhibitors

被引：21

作者：

Gomez, Cindy ^{[1
,2
]}

Bai, Longchuan ^{[1
,3
]}

Zhang, Jian ^{[1
,3
]}

Nikolovska-Coleska, Zaneta ^{[1
,4
]}

Chen, Jianyong ^{[1
,3
]}

Yi, Han ^{[1
,3
]}

Wang, Shaomeng ^{[1
,2
,3
,5
]}

机构：

[1] Univ Michigan, Ctr Canc, Ann Arbor, MI 48109 USA

[2] Univ Michigan, Dept Med Chem, Ann Arbor, MI 48109 USA

[3] Univ Michigan, Dept Internal Med, Ann Arbor, MI 48109 USA

[4] Univ Michigan, Dept Pathol, Ann Arbor, MI 48109 USA

[5] Univ Michigan, Dept Pharmacol, Ann Arbor, MI 48109 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 06期

关键词：

STAT3; Small-molecule inhibitors; Peptidomimetics; Freidinger lactams; SMALL-MOLECULE INHIBITOR; CANCER; TARGETS;

D O I：

10.1016/j.bmcl.2009.01.091

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The STAT3 oncogene is a promising molecular target for the design of a new class of anticancer drugs. In this letter, we describe the design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as novel STAT3 inhibitors. Compound 3 binds to STAT3 with a K-i value of 190 nM and is a promising lead compound for further design and optimization. (C) 2009 Published by Elsevier Ltd.

引用

页码：1733 / 1736

页数：4

共 17 条

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