Discovery, Development, and SAR of Aminothiazoles as LIMK Inhibitors with Cellular Anti-Invasive Properties
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
DOI:10.1021/acs.jmedchem.5b01242
日期:2015.10.22
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.
ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES
申请人:UNIVERSAL DISPLAY CORPORATION
公开号:US20210217970A1
公开(公告)日:2021-07-15
Provided is an Ir compound including a ligand L
A
of
wherein the variables are defined herein.