Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors.

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Suzuki N, Shiota T, Watanabe F, Haga N, Murashi T, Ohara T, Matsuo K, Oomori N, Yari H, Dohi K, Inoue M, Iguchi M, Sentou J, Wada T

Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1601-6. doi: 10.1016/j.bmcl.2011.01.119. Epub 2011 Feb 2.

PubMed ID

21334203 [ View in PubMed

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Abstract

A structure-activity relationship study of 4-anilinopyrimidines for dual EGFR/Her-2 inhibitor has resulted in the identification of 4-anilino-5-alkenyl or 5-alkynyl-6-methylpyrimidine derivatives that have exhibited effective inhibitory activity against both enzymes. The presence of 5-alkenyl or 5-alkynyl moiety bearing terminal hydrophilic group played important role for inhibition of these enzymes. Selected compounds in the series demonstrated some activity against Her-2 dependent cell line (BT474).

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Erlotinib	Epidermal growth factor receptor	IC 50 (nM)	1	N/A	N/A	Details