Document Report Card
Basic Information
ID: ALA4130358
Journal: Eur J Med Chem
Title: Chemoselective synthesis and biological evaluation of arylated 2-(Trifluoromethyl) quinolines as nucleotide pyrophosphatase (NPPs) inhibitors.
Authors: Kuhrt D, Ejaz SA, Afzal S, Khan SU, Lecka J, Sévigny J, Ehlers P, Spannenberg A, Iqbal J, Langer P.
Abstract: A new approach to arylated 2-trifluoromethylquinolines based on novel regioselective Suzuki-Miyaura coupling reactions has been developed. Moreover, site-selective, chemo-selective amination reactions were performed. The new 2-trifluoromethylquinoline derivatives were tested as potential NPPs inhibitors and evaluated for their potential to inhibit two families of ecto-nucleotidases, i.e. NPPs and nucleoside triphosphate diphosphohydrolases (NTPDases). Several derivatives were active on a nanomolecular concentration. The results were validated based on docking studies to study the active binding site of the molecules.
CiteXplore: 28735213