Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.

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Zhang YM, Cockerill S, Guntrip SB, Rusnak D, Smith K, Vanderwall D, Wood E, Lackey K

Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.

Bioorg Med Chem Lett. 2004 Jan 5;14(1):111-4.

PubMed ID

14684309 [ View in PubMed

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Abstract

A series of 6-alkoxy-4-anilinoquinazoline compounds was prepared and evaluated for in vitro inhibition of the erbB2 and EGFR kinase activity. The IC(50) values of the best compounds were below 0.10 uM. Further, several of these compounds inhibit the growth of erbB2 and EGFR over-expressing tumor cell lines at concentrations below 1 uM.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Erlotinib	Epidermal growth factor receptor	IC 50 (nM)	1	7.5	23	Details
Gefitinib	Epidermal growth factor receptor	IC 50 (nM)	1	7.5	23	Details
Lapatinib	Epidermal growth factor receptor	IC 50 (nM)	10	7.5	23	Details