Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently …

…, SK Rabindran, R Nilakantan, LM Greenberger…

Index: Wissner, Allan; Brawner Floyd; Rabindran, Sridhar K.; Nilakantan, Ramaswamy; Greenberger, Lee M.; Shen, Ru; Wang, Yu-Fen; Tsou, Hwei-Ru Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 20 p. 2893 - 2897

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Citation Number: 55

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.