897445-46-4Relevant 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 (2014)
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.
COMPOUNDS USEFUL AS CHEMOKINE RECEPTOR ANTAGONISTS
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Page/Page column 87, (2008/06/13)
The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.
