Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4794-7. doi: 10.1016/j.bmcl.2008.07.093. Epub 2008 Jul 27.

Abstract

The bisamide class of kinase inhibitors was identified as being active against CSF-1R. The synthesis and SAR of pyridyl and thiazolyl bisamides are reported, along with the pharmacokinetic properties and in vivo activity of selected examples.

Publication types

  • Comparative Study

MeSH terms

  • 3T3 Cells
  • Amides / chemistry
  • Amides / pharmacokinetics
  • Amides / pharmacology*
  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / pharmacology*
  • Female
  • Humans
  • Mice
  • Mice, Nude
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism*
  • Rats
  • Receptor, Macrophage Colony-Stimulating Factor / antagonists & inhibitors*
  • Receptor, Macrophage Colony-Stimulating Factor / genetics
  • Thiazoles / chemistry
  • Thiazoles / pharmacokinetics
  • Thiazoles / pharmacology*

Substances

  • Amides
  • Antineoplastic Agents
  • Thiazoles
  • Receptor, Macrophage Colony-Stimulating Factor