Design and Synthesis of 4-(4-Benzoylaminophenoxy) phenol Derivatives As Androgen Receptor Antagonists

…, S Fujii, S Mori, H Kagechika

Index: Yamada, Ayumi; Fujii, Shinya; Mori, Shuichi; Kagechika, Hiroyuki ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 10 p. 937 - 941

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Citation Number: 8

Abstract

We report the design and synthesis of novel 4-(4-benzoylaminophenoxy) phenol derivatives that bind to the androgen receptor (AR) ligand-binding domain and exhibit potent androgen- antagonistic activity. Compound 22 is one of the most potent of these derivatives, inhibiting the dihydrotestosterone-promoted growth of SC-3 cell line bearing wild-type AR (IC50 0.75 μM), LNCaP cell line bearing T877A-mutated AR (IC50 0.043 μM), and 22Rv1 cell line ...