Design and Synthesis of Small and Potent Inhibitors of Urokinase as Antitumor Agents

A set of small nonpeptidic diaryl phosphonate inhibitors was prepared. The phosphonate derivatives were synthesized through Birum-Oleksyszyn reaction followed by reduction of the nitro-group which undergo to Boc-protected guanidine derivatives. After removing of Boc-group by TFAA/DCM afford the guanidine phosphonates.