Fluorophosphonate Derivatives of N9-Benzylguanine as Potent, Slow- Binding Multisubstrate Analogue Inhibitors of Purine Nucleoside Phosphorylase.

Abstract The phosphonate derivatives of N9-benzylguanine (4a–4h) have been prepared as purine nucleoside phophorylase inhibitors. Enzyme inhibition studies with PNP from calf spleen or human erythrocyte show that compounds 4b and 4c are among the best PNP inhibitors ever reported, demonstrating further the importance of fluorines in such type of inhibitors.