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ID: ALA1135208

Journal: Bioorg Med Chem Lett

Title: 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.

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

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.

CiteXplore: 12270171

DOI: 10.1016/s0960-894x(02)00598-x