《Discovery of the Potent Phosphoinositide 3-Kinase d (PI3 K d) Inhibitors》 was written by Lei, Tao; Hong, Yongwei; Chang, Xinyue; Zhang, Zhimin; Liu, Xingguo; Hu, Miao; Huang, Wenhai; Yang, Haiyan. Application In Synthesis of 2-Pyridinylboronic acid And the article was included in ChemistrySelect in 2020. The article conveys some information:
The PI3Kd plays a pivotal role in regulating immune cell function and has recently emerged as a promising therapeutic target in treating various diseases, which draw more and more attention to discover potent PI3Kd inhibitors in recent years. Starting from structure-based drug design, a series of derivatives were designed and synthesized as new chemotypes of PI3Kd inhibitors. The potential compounds were structurally optimized by interaction showed in docking study. In cell-free kinase activity assays, Homogeneous Time-Resolved Fluorescence Assay (HTRF) method was performed for evaluating the inhibitory activities against PI3Kd. Interestingly, the representative compound 4 exhibited potent PI3Kd activity (IC50=72 nM), which is comparable to that of pos. compound TGR1202. Furthermore, compound 4 showed 15-fold water solubility than TGR1202. In addition, the tests of compound 4 on anti-cancer activity against jeko-1 cancer cell line and cytotoxicity against peripheral blood mononuclear cell (PBMC) suggested high inhibition activity and low toxicity resp. A series of experiments indicated that compound 4 possessed novel chem. structure and high-efficiency PI3Kd inhibition activity, deserving further structural optimization to develop highly potent PI3Kd inhibitors. The results came from multiple reactions, including the reaction of 2-Pyridinylboronic acid(cas: 197958-29-5Application In Synthesis of 2-Pyridinylboronic acid)
2-Pyridinylboronic acid(cas: 197958-29-5) belongs to pyridine. When pyridine is adsorbed on oxide surfaces or in porous materials, the following species are commonly observed: (i) pyridine coordinated to Lewis acid sites, (ii) pyridine H-bonded to weakly acidic hydroxyls, and (iii) protonated pyridine. At high coverage, physisorbed pyridine and protonated dimers can also be observed.Application In Synthesis of 2-Pyridinylboronic acid