Tyrosine kinase inhibitors. 16. 6, 5, 6-Tricyclic benzothieno [3, 2-d] pyrimidines and pyrimido [5, 4-b]-and-[4, 5-b] indoles as potent inhibitors of the epidermal growth …

…, H Zhou, AD Sercel, A McMichael, DW Fry

Index: Showalter, H. D. Hollis; Bridges, Alexander J.; Zhou, Hairong; Sercel, Anthony D.; McMichael, Amy; Fry, David W. Journal of Medicinal Chemistry, 1999 , vol. 42, # 26 p. 5464 - 5474

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Citation Number: 108

Abstract

Several elaborations of the fundamental anilinopyrimidine pharmacophore have been reported as potent and selective inhibitors of the epidermal growth factor receptor (EGFr) tyrosine kinase. This paper reports on a series of inhibitors whereby some 6, 5-bicyclic heteroaromatic systems were fused through their C-2 and C-3 positions to this anilinopyrimidine pharmacophore. Although the resulting tricycles did not produce the ...