The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors.
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Graham Robinett R, Freemerman AJ, Skinner MA, Shewchuk L, Lackey K
The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors.
Bioorg Med Chem Lett. 2007 Nov 1;17(21):5886-93. Epub 2007 Aug 25.
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- 17884497 [ View in PubMed]
- 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.