Development of β-amino-carbonyl compounds as androgen receptor antagonists.

ABSTRACT:

Aim

Androgen receptor (AR) antagonists have proven to be useful in the early control of prostate cancer. The aim of this study was to identify and characterize a novel β-amino-carbonyl-based androgen receptor antagonist.

Methods

Different isomers of the β-amino-carbonyl compounds were obtained by chiral separation. The bioactivities of the isomers were evaluated by AR nuclear translocation, mammalian two-hybrid, competitive receptor binding and cell proliferation assays. The expression of genes downstream of AR was analyzed with real-time PCR. The therapeutic effects on tumor growth in vivo were observed in male SCID mice bearing LNCaP xenografts.

Results

Compound 21 was previously identified as an AR modulator by the high-throughput screening of a diverse compound li

SUBMITTER: Zhang ZY 

PROVIDER: S-EPMC4814037 | biostudies-literature | 2014 May

REPOSITORIES: biostudies-literature