709639-84-9Relevant 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.
The first example of the Fischer-Hepp type rearrangement in pyrimidines
Cikotiene, Inga,Jonusis, Mantas,Jakubkiene, Virginija
supporting information, p. 1819 - 1825 (2013/10/22)
A N-nitroso moiety can be used for the activation of chloropyrimidines toward a nucleophilic substitution reaction with amines. The subsequent treatment of the obtained products with aq H2SO4 can lead to either N-denitrosation to obtain 4,6-pyrimidinediamines or to a Fischer-Hepp type rearrangement to obtain 5-nitroso-4,6-pyrimidinediamines. It was found that the outcome of the reaction strongly depends on the structure of the pyrimidines. Activation of the pyrimidine ring by three groups with a positive mesomeric effect is crucial for the intramolecular nitroso group migration.
SOLUBLE GUANYLATE CYCLASE ACTIVATORS
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Page/Page column 62-63, (2011/10/13)
The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds are capable of modulating the body's production of cyclic guanosine monophosphate ("cGMP") and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.
