[EN] HETEROCYCLIC DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF [FR] DÉRIVÉ DE BENZOTHIOPHÈNE, PROCÉDÉ DE PRÉPARATION ASSOCIÉ ET UTILISATION ASSOCIÉE [ZH] 杂环类衍生物及其制备方法和用途
The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors
作者:R. Graham Robinett、Alex J. Freemerman、Michael A. Skinner、Lisa Shewchuk、Karen Lackey
DOI:10.1016/j.bmcl.2007.07.104
日期:2007.11
4-(3-hydroxyanilino)-quinolinecompounds, initially identified as small-molecule inhibitors of src family kinases, have been evaluated as potential inhibitors of RET kinase. Three compounds, 38, 31, and 40, had K(i)'s of 3, 25, and 50 nM in an in vitro kinase assay; while a cell based kinase assay showed K(i)'s of 300, 100, and 45 nM, respectively. These compounds represent potential new leads for the treatment
A derivative, which is useful as a ret kinase inhibitor is described herein. The described invention also includes methods of using the same in the treatment of diseases mediated by inappropriate ret kinase activity.