219840-89-8Relevant academic research and scientific papers
Discovery of 2-(cyclohexylmethylamino)pyrimidines as a new class of reversible valosine containing protein inhibitors
Cervi, Giovanni,Magnaghi, Paola,Asa, Daniela,Avanzi, Nilla,Badari, Alessandra,Borghi, Daniela,Caruso, Michele,Cirla, Alessandra,Cozzi, Liviana,Felder, Eduard,Galvani, Arturo,Gasparri, Fabio,Lomolino, Antonio,Magnuson, Steven,Malgesini, Beatrice,Motto, Ilaria,Pasi, Maurizio,Rizzi, Simona,Salom, Barbara,Sorrentino, Graziella,Troiani, Sonia,Valsasina, Barbara,O'Brien, Thomas,Isacchi, Antonella,Donati, Daniele,D'Alessio, Roberto
, p. 10443 - 10454 (2015/02/19)
Valosine-containing protein (VCP), also known as p97 or cdc48 in yeast, is a highly abundant protein belonging to the AAA ATPase family involved in a number of essential cellular functions, including ubiquitin-proteasome mediated protein degradation, Golgi reassembly, transcription activation, and cell cycle control. Altered expression of VCP has been detected in many cancer types sometimes associated with poor prognosis. Furthermore, VCP mutations are causative of some neurodegenerative disorders. In this paper we report the discovery, synthesis, and structure-activity relationships of substituted 2-aminopyrimidines, representing a new class of reversible VCP inhibitors. This class of compounds, identified in a HTS campaign against recombinant VCP, has been progressively expanded and manipulated to increase biochemical potency and gain cellular activity.
Aryl- and arylamino- substituted heterocycles as corticotropin releasing hormone antagonists
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, (2008/06/13)
Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.
4-Aryl-2-anilinopyrimidines as corticotropin-releasing hormone (CRH) antagonists
Cocuzza, Anthony J.,Hobbs, Frank W.,Arnold, Charles R.,Chidester, Dennis R.,Yarem, Jerry A.,Culp, Steven,Fitzgerald, Lawrence,Gilligan, Paul J.
, p. 1057 - 1062 (2007/10/03)
A series of 4-aryl-2-(N-ethylanilino)pyrimidines has been synthesized as corticotropin-releasing hormone (CH) inhibitors. The effect of substitution on each aromatic ring on receptor binding was investigated.
