Chiral Aromatase and Dual Aromatase− Steroid Sulfatase Inhibitors from the Letrozole Template: Synthesis, Absolute Configuration, and In Vitro Activity†

…, JR Labrosse, MN Trusselle, S Abbate…

文献索引：Wood, Paul M.; Woo, L. W. Lawrence; Labrosse, Jean-Robert; Trusselle, Melanie N.; Abbate, Sergio; Longhi, Giovanna; Castiglioni, Ettore; Lebon, France; Purohit, Atul; Reed, Michael J.; Potter, Barry V. L. Journal of Medicinal Chemistry, 2008 , vol. 51, # 14 p. 4226 - 4238

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被引用次数: 45

摘要

To explore aromatase inhibition and to broaden the structural diversity of dual aromatase− sulfatase inhibitors (DASIs), we introduced the steroid sulfatase (STS) inhibitory pharmacophore to letrozole. Letrozole derivatives were prepared bearing bis-sulfamates or mono-sulfamates with or without adjacent substituents. The most potent of the achiral and racemic aromatase inhibitor was 40 (IC50= 3.0 nM). Its phenolic precursor 39 was ...