Abstract
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.
Highlights
At present, our attention is focused on the COVID-19 pandemic and there is a tendency to neglect the civilization diseases which remain the main reason for mortality worldwide
Research, we reported on on the the synthesis synthesis and and antiproliferative antiproliferative action novel phenolic adducts of of bicyclic bicyclicimine imine11(Scheme (Scheme1)1)[30]
Cyclic imine 1, derived from optically pure trans-(R,R)-1,2-diaminocyclohexane was reacted with HA cyclic imine 1, derived from optically pure trans-(R,R)-1,2-diaminocyclohexane was reacted with phosphonates or phosphine oxides to give compounds 2a–f with good yields as mixtures of epimers
Summary
Our attention is focused on the COVID-19 pandemic and there is a tendency to neglect the civilization diseases which remain the main reason for mortality worldwide. A number of applications such as antiviral [3,4] or cytotoxic agents [5,6], enzyme inhibitors [7,8] immune system activators [9] or antibacterial activities [10] have attracted considerable attention. The importance of these acids and their derivatives in the search for new pharmaceutical uses has been extensively discussed in numerous review articles [11,12,13,14]. The α-aminophosphonic acid and its derivatives pose a crucial role in a variety of biological activities (Figure 1), including cytotoxic properties
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