Discovery, Development, and SAR of Aminothiazoles as LIMK Inhibitors with Cellular Anti-Invasive Properties
详细信息 查看全文
- 作者：Mark D. Charles ; Joanna L. Brookfield ; Tennyson C. Ekwuru ; Martin Stockley ; John Dunn ; Michelle Riddick ; Tim Hammonds ; Elisabeth Trivier ; Gavin Greenland ; Ai Ching Wong ; Anne Cheasty ; Susan Boyd ; Diane Crighton ; Michael F. Olson
- 刊名：Journal of Medicinal Chemistry
- 出版年：2015
- 出版时间：October 22, 2015
- 年：2015
- 卷：58
- 期：20
- 页码：8309-8313
- 全文大小：360K
- ISSN：1520-4804
文摘
As part of a program to develop a small molecule inhibitor of LIMK, a series of aminothiazole inhibitors were discovered by high throughput screening. Scaffold hopping and subsequent SAR directed development led to a series of low nanomolar inhibitors of LIMK1 and LIMK2 that also inhibited the direct biomarker p-cofilin in cells and inhibited the invasion of MDA MB-231-luc cells in a matrigel inverse invasion assay.