Jain, Rama; Mathur, Michelle; Lan, Jiong; Costales, Abran; Atallah, Gordana; Ramurthy, Savithri; Subramanian, Sharadha; Setti, Lina; Feucht, Paul; Warne, Bob; Doyle, Laura; Basham, Stephen; Jefferson, Anne B.; Lindvall, Mika; Appleton, Brent A.; Shafer, Cynthia M. published the artcile< Discovery of Potent and Selective RSK Inhibitors as Biological Probes>, Category: pyrazoles-derivatives, the main research area is difluorophenol pyridine RSK inhibitor preparation antitumor.
While the p90 ribosomal S6 kinase (RSK) family has been implicated in multiple tumor cell functions, the full understanding of this kinase family has been restricted by the lack of highly selective inhibitors. A bis-phenol pyrazole was identified from high-throughput screening as an inhibitor of the N-terminal kinase of RSK2. Structure-based drug design using crystallog., conformational anal., and scaffold morphing resulted in highly optimized difluorophenol pyridine inhibitors of the RSK kinase family as demonstrated cellularly by the inhibition of YB1 phosphorylation. These compounds provide for the first time in vitro tools with an improved selectivity and potency profile to examine the importance of RSK signaling in cancer cells and to fully evaluate RSK as a therapeutic target.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 13808-65-6 belongs to class pyrazoles-derivatives, and the molecular formula is C9H7BrN2, Category: pyrazoles-derivatives.
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics