Tetrahydroindazole inhibitors of CDK2/cyclin complexes was written by Lee, Jae Chul;Hong, Kwon Ho;Becker, Andreas;Tash, Joseph S.;Schonbrunn, Ernst;Georg, Gunda I.. And the article was included in European Journal of Medicinal Chemistry in 2021.Synthetic Route of C6H3BrF3N This article mentions the following:
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 many compounds, for example, 2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0Synthetic Route of C6H3BrF3N).
2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0) belongs to pyridine derivatives. Pyridines are an important class of heterocycles and occur in polysubstituted forms in many naturally occurring biologically active compounds, drug molecules and chiral ligands. Several pyridine derivatives play important roles in biological systems. While its biosynthesis is not fully understood, nicotinic acid (vitamin B3) occurs in some bacteria, fungi, and mammals.Synthetic Route of C6H3BrF3N