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Discovery, Development, and SAR of Aminothiazoles as LIMK Inhibitors with Cellular Anti-Invasive Properties

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NIAID Data Ecosystem2026-03-09 收录
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https://figshare.com/articles/dataset/Discovery_Development_and_SAR_of_Aminothiazoles_as_LIMK_Inhibitors_with_Cellular_Anti_Invasive_Properties/2118727
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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.
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2016-02-12
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