Potent and selective pyrazole-based inhibitors of B-Raf kinase
Herein we describe a novel pyrazole-based class of ATP competitive B-Raf inhibitors. These inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. A subset of these inhibitors has demonstrated the ability to inhibit downstream ERK phosphorylation in LOX tumors from mouse xenograft studies.
Hansen, Joshua D.,Grina, Jonas,Newhouse, Brad,Welch, Mike,Topalov, George,Littman, Nicole,Callejo, Michele,Gloor, Susan,Martinson, Matthew,Laird, Ellen,Brandhuber, Barbara J.,Vigers, Guy,Morales, Tony,Woessner, Rich,Randolph, Nikole,Lyssikatos, Joseph,Olivero, Alan
1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis
Phenotypic whole cell high-throughput screening of a μ150,000 diverse set of compounds against Mycobacterium tuberculosis (Mtb) in cholesterol-containing media identified 1,3-diarylpyrazolyl-acylsulfonamide 1 as a moderately active hit. Structure-activity
Abay, Efrem,Barry, Clifton E.,Basarab, Gregory S.,Boshoff, Helena I. M.,Boyle, Grant A.,Chibale, Kelly,Eyermann, Charles J.,Fienberg, Stephen,Ghorpade, Sandeep R.,Khonde, Lutete Peguy,Lawrence, Nina,Lenaerts, Anne J.,Massoudi, Lisa M.,Myers, Timothy G.,Myrick, Alissa,Nchinda, Aloysius T.,Njoroge, Mathew,Reddy, Virsinha,Robertson, Gregory T.,Singh, Vinayak,Sirgel, Frederick A.,Su, Qin,Van Helden, Paul D.,Müller, Rudolf
p. 12790 - 12807
(2021/09/11)
RAF INHIBITOR COMPOUNDS AND METHODS
Pyrazolyl compounds of Formulas Ia and Ib are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using pyrazolyl compounds for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
-
Page/Page column 82
(2008/06/13)
More Articles about upstream products of 166196-54-9