2. Academic Validation
  3. Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors

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

Affiliation

  • 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.

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