Synthesis of imidazole-derived steroidal hybrids as potent aromatase inhibitors

Imidazolyl substituted 16E-arylidenosteroidal derivatives have been synthesized and evaluated for aromatase inhibitory activity. The steroidal hybrids displayed moderate inhibition of the aromatase enzyme. The enzyme activity was monitored by measuring the tritiated H2O released from [1 beta-H-3] androstenedione during aromatization. 16-[3-{3-(Imidazol-1-yl)propoxy}benzylidene]-4-androstene-3,17-dione (10, IC50: 4.4 mu M) was found to be seven times more potent in comparison to standard drug aminoglutethimide. New imidazolyl substituted 16E-arylidenosteroidal derivatives have been synthesized and evaluated for aromatase inhibitory activity.