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Synthesis and cytostatic activity of 4-bromo-5-ethyl-2-(ethylamino)-5-methyl-5H-1,2-oxaphosphole 2-oxide

Dobromir D. Enchev, Vanya P. Koleva, Asya P. Dragoeva, Leman B. Behchet-Ibryam, Mihail N. Mihaylov, Nikolay M. Uzunov, Laura Melendez-Alafort, Antonio Rosato, Valery Brel.


Recently, much attention has been directed to the synthesis of phosphorus heterocycles. Here we wish to report our results on synthesis and on studying of biological activity of 4-bromo-5-ethyl-2-(ethylamino)-5-methyl-5H-1,2-oxaphosphole 2-oxide (Br-oxph-1) using in vivo and in vitro approaches. Br-oxph-1 represents a structural analogue of 4-bromo-2-(diethylamino)-5-ethyl-5-methyl-5H-1,2-oxaphosphole 2-oxide (Br-oxph). Root growth inhibition test using Triticum aestivum L. seeds was provided in order to determine general toxicity of Br-oxph-1. The effective concentration that cause 50% of root length as compared to control was determined – 8.23×103 μM. Cytotoxic potential of Br-oxph-1 (8.23×103 μM) was evaluated using Allium cepa L.-test. Significant decline in mitotic activity and disturbances of cell cycle kinetics were observed. Further, effects of Br-oxph-1 on human hepatoma cell line SK-HEP-1 in vitro were evaluated by means of cell proliferation assay. The results revealed concentration-dependent and statistically significantinhibitory effect. Concentration of Br-oxph-1 showing 50% reduction in cell proliferation/viability was 0.642×103 µM. In conclusion, plant test-systems used in this study revealed growth inhibitory and cytostatic effects of Br-oxph-1. Data in vitro was in accordance with these results. Results of present study revealed stronger cytostatic effect of Br-oxph-1 in comparison with Br-oxph. Obviously, modifications in chemical structure of Br-oxph influence its biological effects.

Key words: 4-bromo-5-ethyl-2-(ethylamino)-5-methyl-5H-1,2-oxaphosphole 2-oxide, Cytotoxicity, Allium cepa L.-test, WST-1 cell proliferation/viability assay, Cancer cells

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