Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors

Bioorg Med Chem Lett. 2006 May 1;16(9):2419-22. doi: 10.1016/j.bmcl.2006.01.111. Epub 2006 Feb 17.

Abstract

Anilinoalkynylpyrimidines were prepared and evaluated as dual EGFR/ErbB2 kinase inhibitors. A preference was found for substituted phenyl and heteroaromatic rings attached to the alkyne. In addition, the presence of a potential hydrogen bond donor appended to this ring was favored. Selected molecules in the series demonstrated some activity against human tumor cell lines.

MeSH terms

  • Alkynes / chemistry*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Crystallography, X-Ray
  • Drug Screening Assays, Antitumor
  • ErbB Receptors / antagonists & inhibitors*
  • Humans
  • Models, Molecular
  • Molecular Structure
  • Pyrimidines / chemical synthesis
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology*
  • Receptor, ErbB-2 / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • Alkynes
  • Pyrimidines
  • ErbB Receptors
  • Receptor, ErbB-2