Cytotoxic Activity of Piperazin-2-One-Based Structures: Cyclic Imines, Lactams, Aminophosphonates, and Their Derivatives.
N-Heterocycles are considered as desirable scaffolds for the development of novel lead compounds for anticancer drug research. Among them, phosphorus-containing amino-derivatives play a crucial role. A series of imines and products of their further reactions with P-nucleophiles were obtained starting from vicinal bisamines. Reaction of ethylenediamine and α-carbonyl esters yielded in novel unexpected products, which structures were confirmed by crystallographic measurements. The cytotoxic activity evaluation was done on a variety of cell lines including HUH7, AKH12, DAOY, UW228-2, D283, D425, and U251. Human umbilical vein endothelial cells (HUVECs) were used as control. Two of the tested compounds, bearing TADDOL-derived, and trifluoromethyl substituents showed a significant effect on cell viability, though comparable to nonmalignant cells.
['Iwanejko|Jakub|J|', 'Samadaei|Mahzeiar|M|0000-0003-0842-6578', 'Pinter|Matthias|M|0000-0002-7260-532X', 'Senfter|Daniel|D|', 'Madlener|Sibylle|S|', 'Kochel|Andrzej|A|', 'Rohr-Udilova|Nataliya|N|0000-0003-2432-3632', 'Wojaczyńska|Elżbieta|E|0000-0002-1359-0500']
cytotoxic activity cyclic imines aminophosphonates Mannich bases Pudovik reaction viability assay