Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido [3, 4-d] pyrimidines as irreversible inhibitors of the erbB family of tyrosine …

SR Klutchko, H Zhou, RT Winters, TP Tran…

Index: Klutchko, Sylvester R.; Zhou, Hairong; Winters, R. Thomas; Tran, Tuan P.; Bridges, Alexander J.; Althaus, Irene W.; Amato, Danielle M.; Elliott, William L.; Ellis, Paul A.; Meade, Mary Ann; Roberts, Billy J.; Fry, David W.; Gonzales, Andrea J.; Harvey, Patricia J.; Nelson, James M.; Sherwood, Veronica; Han, Hyo-Kyung; Pace, Gerry; Smaill, Jeff B.; Denny, William A.; Showalter, H. D. Hollis Journal of Medicinal Chemistry, 2006 , vol. 49, # 4 p. 1475 - 1485

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Citation Number: 70

Abstract

Structure-activity relationships for inhibition of erbB1, erbB2, and erbB4 were determined for a series of alkynamide analogues of quinazoline-and pyrido [3, 4-d] pyrimidine-based compounds. The compounds were prepared by coupling the appropriate 6- aminoquinazolines or 6-aminopyrido [3, 4-d] pyrimidines with alkynoic acids, using EDCI⊙ HCl in pyridine. The compounds showed pan-erbB enzyme inhibition but were on ...