Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.

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Wissner A, Brawner Floyd MB, Rabindran SK, Nilakantan R, Greenberger LM, Shen R, Wang YF, Tsou HR

Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2893-7.

PubMed ID

12270171 [ View in PubMed

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Abstract

The syntheses and biological evaluations of 4-anilinoquinoline-3-carbonitrile analogues of the three clinical lead 4-anilinoquinazolines Iressa, Tarceva, and CI-1033 are described. The EGFR and HER-2 kinase inhibitory activities and the cell growth inhibition of the two series are compared with each other and with the clinical lead EKB-569. Similar activities are observed between these two series.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Canertinib	Epidermal growth factor receptor	IC 50 (nM)	74	N/A	N/A	Details
Erlotinib	Epidermal growth factor receptor	IC 50 (nM)	1450	N/A	N/A	Details