Synthesis, fluorescence properties and the promising cytotoxicity of pyrene–derived aminophosphonates

• Jarosław Lewkowski,
• Maria Rodriguez Moya,
• Anna Wrona-Piotrowicz,
• Janusz Zakrzewski,
• Renata Kontek and
• Gabriela Gajek

Beilstein J. Org. Chem. 2016, 12, 1229–1235, doi:10.3762/bjoc.12.117

• normal lymphocytes (IC50 = 230.8 µM). Keywords: aminophosphonic derivatives; cytotoxicity; fluorescence properties; MTT test; pyrene-1-carboxaldehyde; Introduction The biological activity of aminophosphonic systems is very well known and described, in aspect of their crop protective [1], antibacterial

• properties. This expectation is supported by the biological activity of azomethine derivatives of pyrene-1-carboxaldehyde. They show antimicrobial action, e.g., 1-phenytoinylacetic acid hydrazone of pyrene-1-carboxaldehyde demonstrated a moderate antimicrobial activity towards Escherichia coli and

• Staphylococcus aureus [14]. Azomethine derivatives of pyrene-1-carboxaldehyde have shown enzyme inhibitory activity, as, e.g., its thiosemicarbazone, which is able to inhibit the action of urease [15]. Although fluorescence properties of pyrene-based aminophosphonic derivatives have been mentioned only once in a