185039-73-0Relevant academic research and scientific papers
Part 3: Notch-sparing γ-secretase inhibitors: SAR studies of 2-substituted aminopyridopyrimidinones
Zhang, Jing,Lu, Dai,Wei, Han-Xun,Gu, Yongli,Selkoe, Dennis J.,Wolfe, Michael S.,Augelli-Szafran, Corinne E.
, p. 2138 - 2141 (2016/04/20)
In search for novel lead compounds as γ-secretase inhibitors, analogs of aminopyrido[2,3-d]pyrimidin-7-ones (I) were synthesized and evaluated for inhibitory effects on amyloid-β-peptide production and cleavage of the Notch1 receptor mediated by γ-secretase. Selected pyridopyrimidines, such as 1, 8, 9,10, 11 and 16 are γ-secretase inhibitors that did not have an effect on Notch1 receptor processing.
2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. Structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity
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.
, p. 3276 - 3292 (2007/10/03)
While engaged in therapeutic intervention against a number of proliferative diseases, we have discovered the 2-aminopyrido[2,3- d]pyrimidin-7(8H)-ones as a novel class of potent, broadly active tyrosine kinase (TK) inhibitors. An efficient route was devel
