Research Article | Volume: 8, Issue: 1, January, 2018

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   

Open Access   

Published:  Jan 28, 2018

DOI: 10.7324/JAPS.2018.8112

Synthesis of phosphorus heterocycles has gained increasing interest in recent years. 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-oxa¬phosphole 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 po¬tential 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 significant inhibitory 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.

Keyword:     4-bromo-5-ethyl-2-(ethylamino)-5-methyl-5H-12- oxaphosphole 2-oxide Cytotoxicity Allium cepa L.-test WST-1 cell proliferation/viability assay Cancer cells


Enchev DD, Koleva VP, Dragoeva AP, Behchet-Ibryam LB, Mihaylov MN, Uzunov NM, Melendez-Alafort L, Rosato A, Brel V. Synthesis and Cytostatic Activity of 4-bromo-5-ethyl2-(ethylamino)-5-methyl-5H-1,2-oxaphosphole 2-oxide. J App Pharm Sci, 2018; 8 (01): 080-086.

Copyright: © The Author(s). This is an open-access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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