Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase
A series of substituted 3-aryl-6-amino-triazolo[4,3-b]pyridazines were identified as highly selective inhibitors of Pim-1 kinase. Initial exploration identified compound 24 as a potent, selective inhibitor, limited in its utility by poor solubility and permeability. Understanding the unusual ATP-binding site of the Pim kinases and X-ray crystallographic data on compound 24 led to design improvements in this class of inhibitor. This resulted in compound 29, a selective, soluble and permeable inhibitor of Pim-1.
Grey, Ron,Pierce, Albert C.,Bemis, Guy W.,Jacobs, Marc D.,Moody, Cameron Stuver,Jajoo, Rahul,Mohal, Narinder,Green, Jeremy
scheme or table
p. 3019 - 3022
(2010/01/16)
STUDIES OF PYRIDAZINE COMPOUNDS, XXV. REINVESTIGATION OF ACYLATION OF PYRIDAZINYLHYDRAZONES
The acylation of morpholino substituted pyridazinylhydrazones afforded triazolopyridazinium salts.Structure elucidation by ir, 1H- and 13C-nmr spectroscopy, reaction mechanism and ring-chain tautomerism are discussed.
Szilagyi, Geza,Matyus, Peter,Sohar, Pal
p. 7921 - 7928
(2007/10/02)
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