TY - JOUR TI - Octahydroquinoxalin-2(1H)-One-Based Aminophosphonic Acids and Their Derivatives—Biological Activity towards Cancer Cells AU - Iwanejko, Jakub AU - Wojaczyńska, Elżbieta AU - Turlej, Eliza AU - Maciejewska, Magdalena AU - Wietrzyk, Joanna T2 - Materials AB - In the search for new antitumor agents, aminophosphonic acids and their derivatives based on octahydroquinoxalin-2(1H)-one scaffold were obtained and their cytotoxic properties and a mechanism of action were evaluated. Phosphonic acid and phosphonate moieties increased the antiproliferative activity in comparison to phenolic Mannich bases previously reported. Most of the obtained compounds revealed a strong antiproliferative effect against leukemia cell line (MV-4-11) with simultaneous low cytotoxicity against normal cell line (mouse fibroblasts-BALB/3T3). The most active compound was diphenyl-[(1R,6R)-3-oxo-2,5-diazabicyclo[4.4.0]dec-4-yl]phosphonate. Preliminary evaluation of the mechanism of action showed the proapoptotic effect associated with caspase 3/7 induction. DA - 2020/01// PY - 2020 DO - 10.3390/ma13102393 DP - www.mdpi.com VL - 13 IS - 10 SP - 2393 LA - en UR - https://www.mdpi.com/1996-1944/13/10/2393 Y2 - 2020/05/29/11:09:07 KW - aminophosphonate KW - antiproliferative activity KW - cell cycle KW - imine KW - mitochondrial membrane potential ER -