Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors

Darren W. Engers, Sean R. Bollinger, Andrew S. Felts, Anish K. Vadukoot, Charles H. Williams, Anna L. Blobaum, Craig W. Lindsley, Charles C. Hong, Corey R. Hopkins

Research output: Contribution to journalArticle

Abstract

The activin-like kinases are a family of kinases that play important roles in a variety of disease states. Of this class of kinases, ALK2, has been shown by a gain-of-function to be the primary driver of the childhood skeletal disease fibrodysplasia ossificans progressiva (FOP) and more recently the pediatric cancer diffuse intrinsic pontine glioma (DIPG). Herein, we report our efforts to identify a novel imidazo[1,2-a]pyridine scaffold as potent inhibitors of ALK2 with good in vivo pharmacokinetic properties suitable for future animal studies.

Original languageEnglish (US)
Article number127418
JournalBioorganic and Medicinal Chemistry Letters
Volume30
Issue number18
DOIs
StatePublished - Sep 15 2020

Keywords

  • ALK2
  • ALK3
  • Activin-like kinase inhibitors
  • BMP inhibitors

ASJC Scopus subject areas

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

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