aminoflavone

Aminoflavone is a synthetic amino-substituted flavone derivative with antineoplastic and antiproliferative activity. It acts primarily as an agonist of the aryl hydrocarbon receptor (AhR), leading to induction of cytochrome P450 enzymes (notably CYP1A1 and CYP1A2) and sulfotransferase SULT1A1. These enzymes bioactivate aminoflavone into reactive metabolites that form DNA adducts, resulting in DNA-protein cross-links, S-phase cell cycle arrest, and apoptosis in cancer cells. Aminoflavone has shown preclinical activity against breast cancer—including tamoxifen-resistant subtypes—by disrupting stemness gene expression and modulating microRNA profiles. The lysyl prodrug form AFP464 is under clinical investigation for advanced solid tumors such as breast cancer[1][5][7][9].

Other names

4H-1-benzopyran-4-one, 5-amino-2-(4-amino-3-fluorophenyl)-6,8-difluoro-7-methyl-aminoflavone prodrug