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.
Alex G Waterson  1 ,  Kirk L Stevens ,  Michael J Reno ,  Yue-Mei Zhang ,  Eric E Boros ,  Frederic Bouvier ,  Abdullah Rastagar ,  David E Uehling ,  Scott H Dickerson ,  Bryan Reep ,  Octerloney B McDonald ,  Edgar R Wood ,  David W Rusnak ,  Krystal J Alligood ,  Sharon K Rudolph
Affiliations
  • 1. GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA. [email protected]
PMID: 16483772 DOI: 10.1016/j.bmcl.2006.01.111
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.