950738-59-7Relevant academic research and scientific papers
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors
Gopalsamy, Ariamala,Ciszewski, Greg,Shi, Mengxiao,Berger, Dan,Hu, Yongbo,Lee, Frederick,Feldberg, Larry,Frommer, Eileen,Kim, Steven,Collins, Karen,Wojciechowicz, Donald,Mallon, Robert
scheme or table, p. 6890 - 6892 (2010/05/19)
Our continued effort towards optimization of the pyrazolo[1,5-a]pyrimidine scaffold as B-Raf kinase inhibitors is described. Structure guided design was utilized to introduce kinase hinge region interacting groups in the 2-position of the scaffold. This s
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors
Berger, Dan M.,Torres, Nancy,Dutia, Minu,Powell, Dennis,Ciszewski, Greg,Gopalsamy, Ariamala,Levin, Jeremy I.,Kim, Kyung-Hee,Xu, Weixin,Wilhelm, James,Hu, YongBo,Collins, Karen,Feldberg, Larry,Kim, Steven,Frommer, Eileen,Wojciechowicz, Donald,Mallon, Robert
scheme or table, p. 6519 - 6523 (2010/05/18)
As part of our research effort to discover B-Raf kinase inhibitors, we prepared a series of C-3 substituted N-(3-(pyrazolo[1,5-a]pyrimidin-7-yl)phenyl)-3-(trifluoromethyl)benzamides. X-ray crystallography studies revealed that one of the more potent inhibitors (10n) bound to B-Raf kinase without forming a hinge-binding hydrogen bond. With basic amine residues appended to C-3 aryl residues, cellular activity and solubility were enhanced over previously described compounds of this class.
Pyrazolo[1,5-A]pyrimidine derivatives and methods of use thereof
-
Page/Page column 25-26; 35; 50, (2010/11/28)
The present invention relates to pyrazolo[1,5-a]pyrimidine derivatives, compositions comprising an effective amount of a pyrazolo[1,5-a]pyrimidine derivative and methods for treating or preventing cancer, comprising administering to a subject in need thereof an effective amount of a pyrazolo[1,5-a]pyrimidine derivative.
Dihydropyrazolo[1,5-A]pyrimidine and dihydroimidazo[1,5-A]pyrimidine derivatives and methods of use thereof
-
Page/Page column 9-10, (2008/06/13)
The present invention relates to dihydropyrazolo[1,5-a]pyrimidine and dihydroimidazo[1,5-a]pyrimidine derivatives, compositions comprising an effective amount of a dihydropyrazolo[1,5-a]pyrimidine or a dihydroimidazo[1,5-a]pyrimidine derivative and method
