Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors.

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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

Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors.

Bioorg Med Chem Lett. 2006 May 1;16(9):2419-22. Epub 2006 Feb 17.

PubMed ID

16483772 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Lapatinib	Epidermal growth factor receptor	IC 50 (nM)	10	N/A	N/A	Details
Lapatinib	Receptor tyrosine-protein kinase erbB-2	IC 50 (nM)	9	N/A	N/A	Details