86626-97-3Relevant academic research and scientific papers
Discovery of Novel Pyrimidine-Based Capsid Assembly Modulators as Potent Anti-HBV Agents
Kim, Woochan,Kang, Jung-Ah,Park, Minji,Jeong, Pyeong-Hwa,Kim, Yoon Jun,Cho, Yuri,Park, Sung-Gyoo,Kim, Yong-Chul
, p. 5500 - 5518 (2021/05/31)
Core assembly modulators of viral capsid proteins have been developed as an effective treatment of chronic hepatitis B virus (HBV) infection. In this study, we synthesized novel potent pyrimidine derivatives as core assembly modulators, and their antivira
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.
Copper-mediated coupling of aminopurines and aminopyrimidines with arylboronic acids
Joshi, Ramesh A.,Patil, Pratap S.,Muthukrishnan,Ramana,Gurjar, Mukund K.
, p. 195 - 197 (2007/10/03)
Selective N-arylation of aminopurines and aminopyrimidines 1-3 with arylboronic acids 4-6 was explored using copper(II) acetate and the corresponding N-arylated purine and pyrimidine derivatives 7-15 were obtained in moderate to good yields.
