2. Academic Validation
  3. The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors

The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors

  • Bioorg Med Chem Lett. 2007 Nov 1;17(21):5886-93. doi: 10.1016/j.bmcl.2007.07.104.
R Graham Robinett 1,  Alex J Freemerman,  Michael A Skinner,  Lisa Shewchuk,  Karen Lackey
Affiliations

Affiliation

  • 1 GlaxoSmithKline, Molecular Discovery Research Chemistry, 5 Moore Drive, Research Triangle Park, NC 27709, USA.
PMID: 17884497 DOI: 10.1016/j.bmcl.2007.07.104
Abstract

Substituted 4-(3-hydroxyanilino)-quinoline compounds, 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 of medullary and papillary thyroid Cancer.

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