C 19-Steroids as androgen receptor modulators: design, discovery, and structure-activity relationship of new steroidal androgen receptor antagonists

P Marwah, A Marwah, HA Lardy, H Miyamoto…

Index: Marwah, Padma; Marwah, Ashok; Lardy, Henry A.; Miyamoto, Hiroshi; Chang, Chawnshang Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 17 p. 5933 - 5947

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Citation Number: 19

Abstract

Dehydroepiandrosterone (DHEA), the most abundant steroid in human circulating blood, is metabolized to sex hormones and other C19-steroids. Our previous collaborative study demonstrated that androst-5-ene-3β, 17β-diol (Adiol) and androst-4-ene-3, 17-dione (Adione), metabolites of DHEA, can activate androgen receptor (AR) target genes. Adiol is maintained at a high concentration in prostate cancer tissue; even after androgen ...