Recommanded Product: 1692-25-7In 2020 ,《Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity》 appeared in European Journal of Medicinal Chemistry. The author of the article were Teng, Yu; Li, Xinyu; Ren, Shengnan; Cheng, Yu; Xi, Kun; Shen, Hongtao; Ma, Wenzhuo; Luo, Guoshun; Xiang, Hua. The article conveys some information:
Herein, a series of quinazoline derivatives I [R1 = Br, 3-pyridyl, (6-fluoro-3-pyridyl), (6-chloro-3-pyridyl), 3-quinolyl; R2 = vinyl, Et, HC=CH2CH3, C≡CCH3; R3 = H, Me] bearing acrylamide fragment were prepared using skeleton-deconstruction strategy. The preliminary bioactivity evaluation resulted in the discovery of lead compound I [R1 = 3-quinolyl; R2 = vinyl; R3 = Me]. Compound I [R1 = 3-quinolyl; R2 = vinyl; R3 = Me] exhibited excellent enzyme activity against PI3Kδ (IC50 = 27.5 nM) compared with BEZ235 as well as the significant anti-proliferation activities. With the high selectivity over other PI3K isoforms and potent effects on PI3K/Akt pathway, compoundI [R1 = 3-quinolyl; R2 = vinyl; R3 = Me] could be identified as a promising PI3Kδ inhibitor worthy of further profiling. The experimental process involved the reaction of Pyridin-3-ylboronic acid(cas: 1692-25-7Recommanded Product: 1692-25-7)
Pyridin-3-ylboronic acid(cas: 1692-25-7) belongs to pyridine. Pyridine and pyridine-derived structures are privileged pharmacophores in medicinal chemistry and an essential functionality for organic chemists. As the prototypical π-deficient heterocycle, pyridine illustrates distinctive chemistry as both substrate and reagent. Recommanded Product: 1692-25-7