Category: pyridine-derivativesIn 2017 ,《Structure-Activity Relationship of Propargylamine-Based HDAC Inhibitors》 was published in ChemMedChem. The article was written by Wuensch, Matthias; Senger, Johanna; Schultheisz, Philipp; Schwarzbich, Sabrina; Schmidtkunz, Karin; Michalek, Carmela; Klass, Michaela; Goskowitz, Stefanie; Borchert, Philipp; Praetorius, Lucas; Sippl, Wolfgang; Jung, Manfred; Sewald, Norbert. The article contains the following contents:
As histone deacetylases (HDACs) play an important role in the treatment of cancer, their selective inhibition has been the subject of various studies. These continuous investigations have given rise to a large collection of pan- and selective HDAC inhibitors, containing diverse US Food and Drug Administration (FDA)-approved representatives. In previous studies, a class of alkyne-based HDAC inhibitors was presented. We modified this scaffold in two previously neglected regions and compared their cytotoxicity and affinity toward HDAC1, HDAC6, and HDAC8. We were able to show that R-configured propargylamines contribute to increased selectivity for HDAC6. Docking studies on available HDAC crystal structures were carried out to rationalize the observed selectivity of the compounds Substitution of the aromatic portion by a thiophene derivative results in high affinity and low cytotoxicity, indicating an improved drug tolerance. In the part of experimental materials, we found many familiar compounds, such as Methyl 5-bromopicolinate(cas: 29682-15-3Category: pyridine-derivatives)
Methyl 5-bromopicolinate(cas: 29682-15-3) 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. Category: pyridine-derivatives