Design, synthesis, and biological evaluation of imidazolyl derivatives of 4, 7-Disubstituted coumarins as aromatase inhibitors selective over 17-α-Hydroxylase/C17− …
The design, synthesis, and biological evaluation of a series of new aromatase (AR, CYP19) inhibitors bearing an imidazole ring linked to a 7-substituted coumarin scaffold at position 4 (or 3) are reported. Many compounds exhibited an aromatase inhibitory potency in the nanomolar range along with a high selectivity over 17-α-hydroxylase/C17− 20 lyase (CYP17). The most potent AR inhibitor was the 7-(3, 4-difluorophenoxy)-4- ...