SYNTHESIS AND STUDY OF THE COVALENT SOLVATION OF 6-NITROAZALOPYRIMIDINES
The corresponding 6-nitroazolopyrimidines were obtained by the reaction of the sodium salt of nitromalondialdehyde with 3(5)-aminotriazoles and 3(5)-aminopyrazoles.The covalent solvation of the synthesized compounds was investigated by PMR spectroscopy.
Rusinov, V. L.,Postovskii, I. Ya.,Petrov, A. Yu.,Sidorov, E. O.,Azev, Yu. A.
Potent and selective pyrazolo[1,5-a]pyrimidine based inhibitors of B-RafV600E kinase with favorable physicochemical and pharmacokinetic properties
Herein we describe a novel series of ATP competitive B-Raf inhibitors based on the pyrazolo[1,5-a]pyrimidine scaffold. These inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. Optimization led to the identification of compound 17, a potent, selective and orally available agent with improved physicochemical and pharmacokinetic properties.
Ren, Li,Laird, Ellen R.,Buckmelter, Alex J.,Dinkel, Victoria,Gloor, Susan L.,Grina, Jonas,Newhouse, Brad,Rasor, Kevin,Hastings, Gregg,Gradl, Stefan N.,Rudolph, Joachim
scheme or table
p. 1165 - 1168
(2012/03/11)
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