Design, synthesis, and biological evaluation of imidazolyl derivatives of 4, 7-Disubstituted coumarins as aromatase inhibitors selective over 17-α-Hydroxylase/C17− …

…, C Zimmer, RW Hartmann, A Carotti

Index: Leonetti, Francesco; Favia, Angelo; Rao, Angela; Aliano, Rosaria; Paluszcak, Anja; Hartmann, Rolf W.; Carotti, Angelo Journal of Medicinal Chemistry, 2004 , vol. 47, # 27 p. 6792 - 6803

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Citation Number: 48

Abstract

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- ...