Lead optimization of 7-benzyloxy 2-(4′-pyridylmethyl) thio isoflavone aromatase inhibitors

…, ES Díaz-Cruz, YW Kim, RW Brueggemeier

Index: Su, Bin; Hackett, John C.; Diaz-Cruz, Edgar S.; Kim, Young-Woo; Brueggemeier, Robert W. Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 23 p. 6571 - 6577

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Citation Number: 27

Abstract

Aromatase, the enzyme responsible for estrogen biosynthesis, is a particularly attractive target in the treatment of hormone-dependent breast cancer. The synthesis and biological evaluation of a series of 2-(4′-pyridylmethyl) thio, 7-alkyl-or aryl-substituted isoflavones as potential aromatase inhibitors are described. The isoflavone derivatives demonstrate IC50 values from 79 to 553nM and compete with the endogenous substrate, androstenedione. ...