Recommanded Product: 1692-25-7In 2022 ,《Design, synthesis and antitumor evaluation of novel quinazoline analogs in hepatocellular carcinoma cell》 appeared in Journal of Molecular Structure. The author of the article were Yu, Pan; Cao, Weiya; Yang, Shilong; Wang, Yuan; Xia, Aixin; Tan, Xinlan; Wang, Luyi. The article conveys some information:
In this paper, five quinazoline analogs I (R = Cl, 1H-indol-5-yl, 4-chlorophenyl, pyridin-3-yl, 4-aminophenyl) were preliminary designed through scaffold shopping from mTOR inhibitors and synthesized in four steps. Five compounds I exhibited potent antitumor activity against the HepG2 cell line by MTT assay. Compound I (R = 1H-indol-5-yl) (II) (IC50 = 4.06μM) was found as the most potent analog and showed better antiproliferative ability than sorafenib (IC50 = 6.14μM). The result of the wound healing assay and transwell migration assay indicated II strong potential to suppress HepG2 cell migration in a dose- and time-dependent manner. The underlying mechanism of its cytotoxicity was also investigated and the results of western blotting confirmed that compound II exposure could block the cell cycle, promote apoptosis and inhibit AKT and mTOR phosphorylation in HepG2 cells. Mol. docking further supported that compound II showed a high affinity to mTOR kinase. The results favored rational design intention and hinted that the new quinazolines I might be helpful in the further explorations of potent agents. In the experimental materials used by the author, we found 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