Name: Pyridin-3-ylboronic acidIn 2020 ,《Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β》 was published in Journal of Medicinal Chemistry. The article was written by Ortega, Jose Antonio; Arencibia, Jose M.; Minniti, Elirosa; Byl, Jo Ann W.; Franco-Ulloa, Sebastian; Borgogno, Marco; Genna, Vito; Summa, Maria; Bertozzi, Sine Mandrup; Bertorelli, Rosalia; Armirotti, Andrea; Minarini, Anna; Sissi, Claudia; Osheroff, Neil; De Vivo, Marco. The article contains the following contents:
We disclose a novel class of 6-amino-tetrahydroquinazoline derivatives that inhibit human topoisomerase II (topoII), a validated target of anticancer drugs. In contrast to topoII-targeted drugs currently in clin. use, these compounds do not act as topoII poisons that enhance enzyme-mediated DNA cleavage, a mechanism that is linked to the development of secondary leukemias. Instead, these tetrahydroquinazolines block the topoII function with no evidence of DNA intercalation. We identified a potent lead compound [compound I (ARN-21934) IC50 = 2μM for inhibition of DNA relaxation, as compared to an IC50 = 120μM for the anticancer drug etoposide] with excellent metabolic stability and solubility This new compound also shows ∼100-fold selectivity for topoIIα over topoβ, a broad antiproliferative activity toward cultured human cancer cells, a favorable in vivo pharmacokinetic profile, and the ability to penetrate the blood-brain barrier. Thus, ARN-21934 is a highly promising lead for the development of novel and potentially safer topoII-targeted anticancer drugs. The experimental part of the paper was very detailed, including the reaction process of Pyridin-3-ylboronic acid(cas: 1692-25-7Name: Pyridin-3-ylboronic acid)
Pyridin-3-ylboronic acid(cas: 1692-25-7) belongs to pyridine. Pyridines, quinolines, and isoquinolines have found a function in almost all aspects of organic chemistry. Pyridine has found use as a solvent, base, ligand, functional group, and molecular scaffold. As structural elements, these moieties are potent electron-deficient groups, metal-directing functionalities, fluorophores, and medicinally important pharmacophores. Name: Pyridin-3-ylboronic acid