C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCθ inhibitors: Part I was written by Subrath, Joan;Wang, Daniel;Wu, Biqi;Niu, Chuansheng;Boschelli, Diane H.;Lee, Julie;Yang, Xiaoke;Brennan, Agnes;Chaudhary, Divya. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2009.Application of 1073354-14-9 This article mentions the following:
We earlier reported that 3-pyridinecarbonitriles with a 4-methylindolyl-5-amino group at C-4 and a Ph group at C-5 were inhibitors of PKCθ. Keeping the group at C-4 of the pyridine core constant, we varied the water solubilizing group on the Ph ring at C-5 and then replaced the C-5 Ph ring with several monocyclic heteroaryl rings, including furan, thiophene and pyridine. Analog 6e (I) with a 4-methylindol-5-ylamino group at C-4 and a 5-[(4-methylpiperazin-1-yl)methyl]-2-furyl group C-5 had an IC50 value of 4.5 nM for the inhibition of PKCθ. In the experiment, the researchers used many compounds, for example, 5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)picolinaldehyde (cas: 1073354-14-9Application of 1073354-14-9).
5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)picolinaldehyde (cas: 1073354-14-9) belongs to pyridine derivatives. The ring atoms in the pyridine molecule are sp2-hybridized. The nitrogen is involved in the π-bonding aromatic system using its unhybridized p orbital. The lone pair is in an sp2 orbital, projecting outward from the ring in the same plane as the σ bonds. Reduced pyridines, namely tetrahydropyridines, dihydropyridines and piperidines, are found in numerous natural and synthetic compounds. The synthesis and reactivity of these compounds have often been driven by the fact many of these compounds have interesting and unique pharmacological properties. Application of 1073354-14-9