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ID: ALA3621108
Journal: J Med Chem
Title: Discovery, Development, and SAR of Aminothiazoles as LIMK Inhibitors with Cellular Anti-Invasive Properties.
Authors: Charles MD, Brookfield JL, Ekwuru TC, Stockley M, Dunn J, Riddick M, Hammonds T, Trivier E, Greenland G, Wong AC, Cheasty A, Boyd S, Crighton D, Olson MF.
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.
CiteXplore: 26356364