Cytotoxic activity of N, N'-Bis (2-hydroxybenzyl) ethylenediamine derivatives in human cancer cell lines.

BACKGROUND Compounds containing ethylenediamine (-NCH2CH2N-) moiety are known to exhibit antimicrobial, -fungal, -bacterial, -tuberculosis and -cancer activities. MATERIALS AND METHODS In the present study, we evaluated the in vitro cytotoxic activity of N,N'-bis(2-hydroxybenzyl)- (6), N,N'-bis(5-bromo-2-hydroxybenzyl)- (7) and N,N'-bis(5-chloro-2-hydroxybenzyl) (8)- ethylenediamine dihydrochlorides; and N,N'-bis(2-hydroxybenzyl)- (9), N,N'-bis(5-bromo-2-hydroxybenzyl)- (10) and N,N'-bis(5-chloro-2-hydroxybenzyl) (11)- ethylenediamine toward human lung (A549), breast (MDA-MB-231) and prostate (PC3) cancer cell lines after 24-h treatment using crystal violet dye binding assay. Effects on the cell cycle the using flow cytometry, and mitochondrial membrane potential using rhodamine-123 florescent dye were also evaluated. RESULTS Compounds 7 and 8 exhibit cytotoxic activity, causing cell arrest at different phases of the cell cycle and loss of mitochondrial membrane potential in the above cancer cell lines. CONCLUSION These findings clearly demonstrate, to our knowledge for the first time, that ethylenediamine dihydrochloride salts-compounds 7 and 8-exhibit concentration-dependent cytotoxic activity towards A549, MDA-MB-231 and PC3 cancer cell lines, which may serve as a basis for future work on novel therapeutic agents.