488816-96-2Relevant academic research and scientific papers
Redox deracemization of phosphonate-substituted dihydropyrimidines
Feng, Guang-Shou,Guo, Xuan,Meng, Fan-Jie,Shao, Bing-Ru,Shi, Lei,Velopolcek, Maria K.
supporting information, p. 10570 - 10574 (2021/12/27)
An efficient redox deracemization of the phosphonic ester substituted 3,4-dihydropyrimidin-2-one (DHPM) derivatives is described. The one-pot deracemization strategy consisted of the oxidization to destroy the stereocenter center and the following asymmetric transfer hydrogenation to regenerate the chiral carbon center with the vicinal phosphonic ester group, providing a series of optically active phosphonate substituted DHPMs with up to 96% ee.
Pyrimidine bis-aromatic ring derivative epidermal growth factor inhibitor, and preparation method and application thereof
-
Paragraph 0214-0218, (2020/09/09)
The invention relates to a pyrimidine double-aromatic-ring derivative epidermal growth factor inhibitor, and a preparation method and application thereof. The invention discloses a selective inhibitorfor a clinical mutant of EGFR protein tyrosine kinase.
Design of new quinolin-2-one-pyrimidine hybrids as sphingosine kinases inhibitors
Abonia, Rodrigo,Andújar, Sebastián,Cobo, Justo,Enriz, Ricardo D.,Gutiérrez, Lucas,Insuasty, Daniel,Lima, Santiago,Marchal, Antonio,Nogueras, Manuel,Spiegel, Sarah,Vettorazzi, Marcela
, (2019/12/09)
Sphingosine-1-phosphate is now emerging as an important player in cancer, inflammation, autoimmune, neurological and cardiovascular disorders. Abundance evidence in animal and humans cancer models has shown that SphK1 is linked to cancer. Thus, there is a
Hit to lead studies on (hetero)arylpyrimidines-Agonists of the canonical Wnt-β-catenin cellular messaging system
Gilbert, Adam M.,Bursavich, Matthew G.,Alon, Nippa,Bhat, Bheem M.,Bex, Frederick J.,Cain, Michael,Coleburn, Valerie,Gironda, Virginia,Green, Paula,Hauze, Diane B.,Kharode, Yogendra,Krishnamurthy, Girija,Kirisits, Matthew,Lam, Ho-Sun,Liu, Yao-Bin,Lombardi, Sabrina,Matteo, Jeanne,Murrills, Richard,Robinson, John A.,Selim, Sally,Sharp, Michael,Unwalla, Raymond,Varadarajan, Usha,Zhao, Weiguang,Yaworsky, Paul J.
scheme or table, p. 366 - 370 (2010/04/06)
A series of (hetero)arylpyrimidines agonists of the Wnt-β-catenin cellular messaging system have been prepared. These compounds show activity in U2OS cells transfected with Wnt-3a, TCF-luciferase, Dkk-1 and tk-Renilla. Selected compounds show minimal GSK-3β inhibition indicating that the Wnt-β-catenin agonism activity most likely comes from interaction at Wnt-3a/Dkk-1. Two examples 1 and 25 show in vivo osteogenic activity in a mouse calvaria model. One example 1 is shown to activate non-phosphorylated β-catenin formation in bone.
(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: A wingless β-catenin agonist that increases bone formation rate
Pelletier, Jeffrey C.,Lundquist IV, Joseph T.,Gilbert, Adam M.,Alon, Nipa,Bex, Frederick J.,Bhat, Bheem M.,Bursavich, Mattew G.,Coleburn, Valerie E.,Felix, Luciana A.,Green, Daniel M.,Green, Paula,Hauze, Diane B.,Kharode, Yogendra P.,Lam, Ho-Sun,Lockhead, Susan R.,Magolda, Ronald L.,Matteo, Jeanne J.,Mehlmann, John F.,Milligan, Colleen,Murrills, Richard J.,Pirrello, Jennifer,Selim, Sally,Sharp, Michael C.,Unwalla, Ray J.,Vera, Matthew D.,Wrobel, Jay E.,Yaworsky, Paul,Bodine, Peter V. N.
supporting information; experimental part, p. 6962 - 6965 (2010/08/03)
A high-throughput screening campaign to discover small molecule leads for the treatment of bone disorders concluded with the discovery of a compound with a 2-aminopyrimidine template that targeted the Wnt β-catenin cellular messaging system. Hit-tolead in
HETEROARYL/ARYL PYRIMIDINE ANALOGS AND THEIR USE AS AGONISTS OF THE WNT-BETA-CATENIN CELLULAR MESSAGING SYSTEM
-
Page/Page column 27, (2008/12/09)
The present invention relates to heteroaryl/aryl pyrimidine analogs, methods of making aryl/heteroaryl pyrimidine analogs, compositions comprising a aryl/heteroaryl pyrimidine analog, and methods for treating canonical Wnt-β-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of a heteroaryl/aryl pyrimidine analog.
