Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors.

Waterson AG, Stevens KL, Reno MJ, Zhang YM, Boros EE, Bouvier F, Rastagar A, Uehling DE, Dickerson SH, Reep B, McDonald OB, Wood ER, Rusnak DW, Alligood KJ, Rudolph SK
Bioorg Med Chem Lett. 2006 16 (9): 2419-22

PMID: 16483772 · DOI:10.1016/j.bmcl.2006.01.111

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 (12)

Alkynes Cell Line, Tumor Cell Proliferation Crystallography, X-Ray Drug Screening Assays, Antitumor ErbB Receptors Humans Models, Molecular Molecular Structure Pyrimidines Receptor, ErbB-2 Structure-Activity Relationship

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