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Synthesis and evaluation of 4-(2-pyrimidinylamino) benzamides inhibitors of hedgehog signaling pathway

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
24
Issue
3
Identifiers
DOI: 10.1016/j.bmcl.2013.12.050
Keywords
  • Hedgehog Signaling Pathway
  • Inhibitors
  • Sar
  • Pharmacokinetic Properties
Disciplines
  • Chemistry
  • Design
  • Pharmacology

Abstract

Graphical abstract A novel series of hedgehog signaling pathway inhibitors has been designed based on the 4-(2-pyrimidinylamino) benzamides scaffold. The synthesis and SAR of these compounds are described. Optimization leads to the identification of compound 3c, a potent and orally available agent with improved physicochemical and pharmacokinetic properties.

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