2. Academic Validation
  3. 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

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. doi: 10.1016/s0960-894x(02)00598-x.
Allan Wissner 1,  M Brawner Brawner Floyd,  Sridhar K Rabindran,  Ramaswamy Nilakantan,  Lee M Greenberger,  Ru Shen,  Yu-Fen Wang,  Hwei-Ru Tsou
Affiliations

Affiliation

  • 1 Chemical Sciences and Oncology and Immunoinflammatory Research, Wyeth Research, 401N. Middletown Road, Pearl River, NY 10965, USA. [email protected]
PMID: 12270171 DOI: 10.1016/s0960-894x(02)00598-x
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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