Emanuele Fabbrizi

Simplification and Derivatization of Quinoline-Containing M41 Lead to the Discovery of NADPH Oxidase Isoform-Selective Inhibitors Effective in Cancer Cells

Abstract NADPH oxidases (NOXs) are attractive but challenging drug targets. Starting from M41 and its analog MC4876, we synthesized quinoline-based derivatives. SAR studies revealed that modifications at the quinoline C2 position and the amine-moiety influenced potency and isofor...

MolecularStriptease of a Thiadiazolopyrimidine HitYields a Streamlined, Artifact-Free NADPH Mimic for NOX Inhibition

Abstract The convergence of oxidative stress and inflammation drives neurodegeneration and cancer, positioning NADPH oxidases (NOXs) as critical therapeutic targets. Starting from the polyfunctional thiadiazolopyrimidine hit 1, we systematically truncated its peripheral arms to m...