Discovery, development, and SAR of aminothiazoles as LIMK inhibitors with cellular anti-invasive properties

Charles, M. D. et al. (2015) Discovery, development, and SAR of aminothiazoles as LIMK inhibitors with cellular anti-invasive properties. Journal of Medicinal Chemistry, 58(20), pp. 8309-8313. (doi: 10.1021/acs.jmedchem.5b01242) (PMID:26356364)

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Abstract

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.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Crighton, Dr Diane and Olson, Professor Michael
Authors: Charles, M. D., Brookfield, J. L., Ekwuru, T. C., Stockley, M., Dunn, J., Riddick, M., Hammonds, T., Trivier, E., Greenland, G., Wong, A. C., Cheasty, A., Boyd, S., Crighton, D., and Olson, M. F.
College/School:College of Medical Veterinary and Life Sciences > School of Cancer Sciences
Journal Name:Journal of Medicinal Chemistry
Publisher:American Chemical Society
ISSN:0022-2623
ISSN (Online):1520-4804
Published Online:10 September 2015
Copyright Holders:Copyright © 2015 American Chemical Society
First Published:First published in Journal of Medicinal Chemistry 58(20):8309-8313
Publisher Policy:Reproduced in accordance with the copyright policy of the publisher

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