New alkyl imidazoline derivatives have been synthesized as potential anticancer agents. The antiproliferative activity of these compounds, evaluated against representative human haematological and solid neoplastic cell lines, showed that N, N′-di (4,5-dihydro-1H-imidazol-2-yl)3-aza-1,10-decane- diamine (8) and N, N′-di (4,5-dihydro-1H-imidazol-2-yl)3-aza-1,10- dodecane-diamine (9) were the most active compounds; in fact, they inhibited the cell proliferation at submicromolar concentrations. In enzyme assays, compound 9 turned out to be an inhibitor of topoisomerase II at concentrations comparable with those of the reference topoisomerase II inhibitor, etoposide. © 2006 The Authors.
N, N′ (4,5-dihydro-1H-imidazol-2-yl)3-aza-1,10-decane-diamine and N, N′(4,5-dihydro-1H-imidazol-2-yl)3-aza-1, 10-dodecane-diamine antagonize cell proliferation as selective ligands towards topoisomerase II
Filosa R.
;
2006-01-01
Abstract
New alkyl imidazoline derivatives have been synthesized as potential anticancer agents. The antiproliferative activity of these compounds, evaluated against representative human haematological and solid neoplastic cell lines, showed that N, N′-di (4,5-dihydro-1H-imidazol-2-yl)3-aza-1,10-decane- diamine (8) and N, N′-di (4,5-dihydro-1H-imidazol-2-yl)3-aza-1,10- dodecane-diamine (9) were the most active compounds; in fact, they inhibited the cell proliferation at submicromolar concentrations. In enzyme assays, compound 9 turned out to be an inhibitor of topoisomerase II at concentrations comparable with those of the reference topoisomerase II inhibitor, etoposide. © 2006 The Authors.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
