23659-45-2Relevant articles and documents
Fragment-based drug design of novel pyranopyridones as cell active and orally bioavailable tankyrase inhibitors
De Vicente, Javier,Tivitmahaisoon, Parcharee,Berry, Pamela,Bolin, David R.,Carvajal, Daisy,He, Wei,Huang, Kuo-Sen,Janson, Cheryl,Liang, Lena,Lukacs, Christine,Petersen, Ann,Qian, Hong,Yi, Lin,Zhuang, Yong,Hermann, Johannes C.
supporting information, p. 1019 - 1024 (2015/09/22)
Tankyrase activity has been linked to the regulation of intracellular axin levels, which have been shown to be crucial for the Wnt pathway. Deregulated Wnt signaling is important for the genesis of many diseases including cancer. We describe herein the discovery and development of a new series of tankyrase inhibitors. These pyranopyridones are highly active in various cell-based assays. A fragment/structure based optimization strategy led to a compound with good pharmacokinetic properties that is suitable for in vivo studies and further development.
Synthesis and some transformations of 4-aryl-substituted amines of the tetrahydropyran series
Arutyunyan,Akopyan,Akopyan,Panosyan,Gevorgyan
experimental part, p. 115 - 119 (2011/04/25)
The reaction of 2-isopropyltetrahydropyran-4-one [obtained by isomerization and hydration of 3-isopropylpent-1-en-4-yn-3-ol in the presence of 5% sulfuric acid and mercury(II) sulfate] with ethyl cyanoacetate gave ethyl cyano(2-isopropyltetrahydropyran-4-
