1201361-75-2Relevant academic research and scientific papers
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors
Katz, Jason D.,Haidle, Andrew,Childers, Kaleen K.,Zabierek, Anna A.,Jewell, James P.,Hou, Yongquan,Altman, Michael D.,Szewczak, Alexander,Chen, Dapeng,Harsch, Andreas,Hayashi, Mansuo,Warren, Lee,Hutton, Michael,Nuthall, Hugh,Su, Hua-Poo,Munshi, Sanjeev,Stanton, Matt G.,Davies, Ian W.,Munoz, Ben,Northrup, Alan
, p. 114 - 120 (2017)
The initial structure activity relationships around an isoindoline uHTS hit will be described. Information gleaned from ligand co-crystal structures allowed for rapid refinements in both MARK potency and kinase selectivity. These efforts allowed for the identification of a compound with properties suitable for use as an in vitro tool compound for validation studies on MARK as a viable target for Alzheimer's disease.[Figure presented]
5,7-DIHYDRO-6H-PYRROLO[2,3-D]PYRIMIDIN-6-ONE DERIVATIVES FOR MARK INHIBITION
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Page/Page column 43-44, (2010/01/07)
Compounds of formula I: are potent and selective inhibitors of microtubule affinity regulating kinase (MARK), and hence find use in treatment of Alzheimer's disease and other conditions associated with hyperphosphorylation of tau.
