2-Substituted aminopyrido [2, 3-d] pyrimidin-7 (8 H)-ones. Structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity

…, RW Steinkampf, DL Driscoll, JM Nelson…

Index: Klutchko, Sylvester R.; Hamby, James M.; Boschelli, Diane H.; Wu, Zhipei; Kraker, Alan J.; Amar, Aneesa M.; Hartl, Brian G.; Shen, Cynthia; Klohs, Wayne D.; Steinkampf, Randall W.; Driscoll, Denise L.; Nelson, James M.; Elliott, William L.; Roberts, Billy J.; Stoner, Chad L.; Vincent, Patrick W.; Dykes, Donald J.; Panek, Robert L.; Lu, Gina H.; Major, Terry C.; Dahring, Tawny K.; Hallak, Hussein; Bradford, Laura A.; Showalter, H. D. Hollis; Doherty, Annette M. Journal of Medicinal Chemistry, 1998 , vol. 41, # 17 p. 3276 - 3292

Full Text: HTML

Citation Number: 150

Abstract

While engaged in therapeutic intervention against a number of proliferative diseases, we have discovered the 2-aminopyrido [2, 3-d] pyrimidin-7 (8 H)-ones as a novel class of potent, broadly active tyrosine kinase (TK) inhibitors. An efficient route was developed that enabled the synthesis of a wide variety of analogues with substitution on several positions of the template. From the lead structure 2, a series of analogues bearing variable substituents at ...