Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.

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Hennequin LF, Ballard P, Boyle FT, Delouvrie B, Ellston RP, Halsall CT, Harris CS, Hudson K, Kendrew J, Pease JE, Ross HS, Smith P, Vincent JL

Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.

Bioorg Med Chem Lett. 2006 May 15;16(10):2672-6. Epub 2006 Mar 3.

PubMed ID

16516473 [ View in PubMed

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Abstract

The structure-activity relationship of a novel subseries of 4-anilinoquinazoline EGFR inhibitors substituted at the C-6 position with carbon-linked side chains has been investigated. This exploration has led to the discovery of novel aminomethyl carboxamides with good biological, pharmacokinetic and physical properties.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Gefitinib	Epidermal growth factor receptor	IC 50 (nM)	33	N/A	N/A	Details