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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| Authors: | Wissner Allan Brawner Floyd M Brawner Rabindran Sridhar K Nilakantan Ramaswamy Greenberger Lee M Shen Ru Wang Yu-Fen Tsou Hwei-Ru |
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| Institution: | Chemical Sciences and Oncology and Immunoinflammatory Research, Wyeth Research, 401N. Middletown Road, Pearl River, NY 10965, USA. wissnea@wyeth.com |
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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. |
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