Antitumor agents 222. Synthesis and anti-androgen activity of new diarylheptanoids

…, T Chiang, E Chang, YF Lee, SY Chiu, C Chang…

文献索引：Ohtsu, Hironori; Itokawa, Hideji; Xiao, Zhiyan; Su, Ching-Yuan; Shih, Charles C.-Y.; Chiang, Tzuying; Chang, Eugene; Lee, YiFen; Chiu, Shang-Yi; Chang, Chawnshang; Lee, Kuo-Hsiung Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 23 p. 5083 - 5090

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被引用次数: 51

摘要

Fifteen new diarylheptanoids were synthesized and evaluated for antagonistic activity against androgen receptor (AR)-mediated reporter gene transcription using DU145, PC-3, and LNCaP prostate cancer cell lines. Most compounds showed activity in a 5α- dihydrotestosterone (DHT)-induced reporter gene expression assay in DU145 cells transfected with wild-type AR. Ten compounds (5, 8, 10, 14–15, and 18–22) were ...