Lei, Tao published the artcileDiscovery of the Potent Phosphoinositide 3-Kinase d (PI3 K d) Inhibitors, SDS of cas: 197958-29-5, the publication is ChemistrySelect (2020), 5(1), 196-200, database is CAplus.
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.
ChemistrySelect published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, SDS of cas: 197958-29-5.
Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem