1313519-40-2Relevant academic research and scientific papers
Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors
Bowers, Simeon,Truong, Anh P.,Ye, Michael,Aubele, Danielle L.,Sealy, Jennifer M.,Neitz, R. Jeffrey,Hom, Roy K.,Chan, Wayman,Dappen, Michael S.,Galemmo Jr., Robert A.,Konradi, Andrei W.,Sham, Hing L.,Zhu, Yong L.,Beroza, Paul,Tonn, George,Zhang, Heather,Hoffman, Jennifer,Motter, Ruth,Fauss, Donald,Tanaka, Pearl,Bova, Michael P.,Ren, Zhao,Tam, Danny,Ruslim, Lany,Baker, Jeanne,Pandya, Deepal,Diep, Linnea,Fitzgerald, Kent,Artis, Dean R.,Anderson, John P.,Bergeron, Marcelle
, p. 2743 - 2749 (2013/07/19)
Polo-like kinase-2 (Plk-2) is a potential therapeutic target for Parkinson's disease and this Letter describes the SAR of a series of dihydropteridinone based Plk-2 inhibitors. By optimizing both the N-8 substituent and the biaryl region of the inhibitors we obtained single digit nanomolar compounds such as 37 with excellent selectivity for Plk-2 over Plk-1. When dosed orally in rats, compound 37 demonstrated a 41-45% reduction of pS129-α-synuclein levels in the cerebral cortex.
PTERIDINONES AS INHIBITORS OF POLO - LIKE KINASE
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Page/Page column 169, (2011/07/09)
The present invention provides compounds having a structure according to Formula (I) or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
