Novel N-(phosphonomethyl) glycine derivatives: Design, characterization and biological activity

A series of Cα,α-disubstituted cyclic derivatives of N-(phosphonomethyl) glycine have been synthesized and characterized. They exhibited moderate clastogenicity, low antiproliferative activity on mice bone marrow cells and well expressed cytotoxicity against human tumor cell lines. The 8- and 12-membered cyclic analogs proved superior to the remaining compounds and were found to trigger apoptotic cell death in DOHH-2 cells. The latter compound caused 50% inhibition of the viability of hemobastose-derived cell lines at concentrations ranging from 20 to 67 μM.

Graphical abstractA series of Cα,α-disubstituted cyclic derivatives of N-(phosphonomethyl) glycine have been synthesized and characterized. The results from this study unambiguously indicate that the new aminophosphonates exert antineoplastic potential, combined with low clastogenicity.Figure optionsDownload full-size imageDownload as PowerPoint slide