Cytotoxic Activity Of Piperazin-2-One-Based Structures: Cyclic Imines, Lactams, Aminophosphonates, And Their Derivatives
MATERIALS(2021)
摘要
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 alpha-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.
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关键词
aminophosphonates, cyclic imines, cytotoxic activity, Mannich bases, Pudovik reaction, viability assay
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