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Octahydroquinoxalin-2(1H)-One-Based Aminophosphonic Acids and Their Derivatives-Biological Activity Towards Cancer Cells.

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.

SUBMITTER: Iwanejko J

PROVIDER: S-EPMC7287629 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature

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Octahydroquinoxalin-2(1<i>H</i>)-One-Based Aminophosphonic Acids and Their Derivatives-Biological Activity Towards Cancer Cells.

Iwanejko Jakub J Wojaczyńska Elżbieta E Turlej Eliza E Maciejewska Magdalena M Wietrzyk Joanna J

Materials (Basel, Switzerland) 20200522 10

In the search for new antitumor agents, aminophosphonic acids and their derivatives based on octahydroquinoxalin-2(1<i>H</i>)-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 lo ...[more]

PMID: 32455965

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