Electric Literature of C6H6BrNIn 2021 ,《Tetrahydroindazole inhibitors of CDK2/cyclin complexes》 was published in European Journal of Medicinal Chemistry. The article was written by Lee, Jae Chul; Hong, Kwon Ho; Becker, Andreas; Tash, Joseph S.; Schonbrunn, Ernst; Georg, Gunda I.. The article contains the following contents:
Over 50 tetrahydroindazoles I [R = 2-pyridyl, thiazol-2-yl, pyrimidin-4-yl, etc.] were synthesized after I [R = 2-pyridyl] was identified as a hit compound in a high throughput screen for inhibition of CDK2 in complex with cyclin A. The activity of the most promising analogs was evaluated by inhibition of CDK2 enzyme complexes with various cyclins. Analogs I [R = thiazol-2-yl, pyrimidin-4-yl] showed 3-fold better binding affinity for CDK2 and 2- to 10-fold improved inhibitory activity against CDK2/cyclin A1, E, and O compared to screening hit 3. The data from the enzyme and binding assays indicate that the binding of the analogs to a CDK2/cyclin complex is favored over binding to free CDK2. Computational anal. was used to predict a potential binding site at the CDK2/cyclin E1 interface. In the experiment, the researchers used 2-Bromo-5-methylpyridine(cas: 3510-66-5Electric Literature of C6H6BrN)
2-Bromo-5-methylpyridine(cas: 3510-66-5) 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. Electric Literature of C6H6BrN