Formula: C9H15BN2O2In 2016 ,《Optimization of tetrahydronaphthalene inhibitors of Raf with selectivity over hERG》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Huang, Shih-Chung; Adhikari, Sharmila; Afroze, Roushan; Brewer, Katherine; Calderwood, Emily F.; Chouitar, Jouhara; England, Dylan B.; Fisher, Craig; Galvin, Katherine M.; Gaulin, Jeffery; Greenspan, Paul D.; Harrison, Sean J.; Kim, Mi-Sook; Langston, Steven P.; Ma, Li-Ting; Menon, Saurabh; Mizutani, Hirotake; Rezaei, Mansoureh; Smith, Michael D.; Zhang, Dong Mei; Gould, Alexandra E.. The article contains the following contents:
Investigations of a biaryl ether scaffold identified tetrahydronaphthalene Raf inhibitors with good in vivo activity; however these compounds had affinity toward the hERG potassium channel. Herein the authors describe the work to eliminate this hERG activity via alteration of the substituents on the benzoic amide functionality. The resulting compounds I [R = H, Me2NCH2, MeNHCH2, etc.] have improved selectivity against the hERG channel, good pharmacokinetic properties and potently inhibit the Raf pathway in vivo. In the experiment, the researchers used 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Formula: C9H15BN2O2)
3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Formula: C9H15BN2O2
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics