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

R. Graham Robinett, Alex J. Freemerman, Michael A. Skinner, Lisa Shewchuk, Karen Lackey

Research output: Contribution to journalArticlepeer-review

20 Scopus citations

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 Ki's of 3, 25, and 50 nM in an in vitro kinase assay; while a cell based kinase assay showed Ki's of 300, 100, and 45 nM, respectively. These compounds represent potential new leads for the treatment of medullary and papillary thyroid cancer.

Original languageEnglish (US)
Pages (from-to)5886-5893
Number of pages8
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number21
DOIs
StatePublished - Nov 1 2007

Keywords

  • 4-Anilinoquinolines
  • Kinase inhibitors
  • RET
  • c-src

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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