Discovery of Potent and Selective RSK Inhibitors as Biological Probes was written by 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.. And the article was included in Journal of Medicinal Chemistry in 2015.Electric Literature of C7H5BrF2O This article mentions the following:
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. In the experiment, the researchers used many compounds, for example, 4-Bromo-2,6-difluoroanisole (cas: 104197-14-0Electric Literature of C7H5BrF2O).
4-Bromo-2,6-difluoroanisole (cas: 104197-14-0) belongs to ethers. Ether is less polar than esters, alcohols or amines because of the oxygen atom that is unable to participate in hydrogen bonding due to the presence of bulky alkyl groups on both sides of the oxygen atom. But ether is more polar than alkenes. Ethers feature bent C–O–C linkages. In dimethyl ether, the bond angle is 111° and C–O distances are 141 pm. The barrier to rotation about the C–O bonds is low. The bonding of oxygen in ethers, alcohols, and water is similar. In the language of valence bond theory, the hybridization at oxygen is sp3.Electric Literature of C7H5BrF2O
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem