In 2014,Hu, Ping; Wang, Xinghui; Zhang, Baiqun; Zhang, Shuai; Wang, Qiang; Wang, Zhiyong published 《Fluorescence Polarization for the Evaluation of Small-Molecule Inhibitors of PCAF BRD/Tat-AcK50 Association》.ChemMedChem published the findings.Reference of 5-Bromo-2-chloropyridine The information in the text is summarized as follows:
A fluorescence polarization competitive assay was developed to efficiently screen and evaluate inhibitors of PCAF bromodomain/Tat-AcK50 protein-peptide interaction. A series of pyridine 1-oxide derivatives were synthesized and evaluated. Some of the novel compounds, 2-(3-aminopropylamino) pyridine 1-oxide derivatives, could be effective inhibitors of PCAF bromodomain/Tat-AcK50 association Specifically, 2-(3-aminopropylamino)-5-(hydroxymethyl)pyridine 1-oxide hydrochloride (15) and the 5-((3-aminopropylamino)methyl) derivative (20) were found to be effective ligands for the PCAF BRD pocket. First preliminary cellular studies indicate that these small-mol. inhibitors have lower cytotoxicities and are potential leads for the anti-HIV/AIDS therapeutic strategy by targeting host-cell protein PCAF BRD to block HIV replication. The results came from multiple reactions, including the reaction of 5-Bromo-2-chloropyridine(cas: 53939-30-3Reference of 5-Bromo-2-chloropyridine)
5-Bromo-2-chloropyridine(cas: 53939-30-3) belongs to pyridine. Pyridine is very deactivated towards electrophilic substitution with respect to benzene. For this reason classical formylation, using methods such as the Gattermann or Vilsmeier reactions, are not generally successful. Reference of 5-Bromo-2-chloropyridine