- Part 3: Notch-sparing γ-secretase inhibitors: SAR studies of 2-substituted aminopyridopyrimidinones
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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.
- Zhang, Jing,Lu, Dai,Wei, Han-Xun,Gu, Yongli,Selkoe, Dennis J.,Wolfe, Michael S.,Augelli-Szafran, Corinne E.
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p. 2138 - 2141
(2016/04/20)
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- PYRIDOPYRIMIDINE KINASE INHIBITORS
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The present invention provides compounds of formula (0): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (0) and provides methods of treat
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- 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
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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
- 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.
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p. 3276 - 3292
(2007/10/03)
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