title: Antitumor agents 222. Synthesis and anti-androgen activity of new diarylheptanoids.
abstract: 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 5alpha-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 equipotent with hydroxyflutamide (HF), the anti-androgen currently available for the treatment of prostate cancer. However, except for compounds 5 and 10, none of the tested compounds was significantly effective in attenuating DHT-induced reporter gene expression in LNCaP cells, which contain endogenous mutant AR.
authors: Natural Products Laboratory, School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599-7360, USA.
authors: Hironori
authors: H
authors: Ohtsu
authors: Hideji
authors: H
authors: Itokawa
authors: Zhiyan
authors: Z
authors: Xiao
authors: Ching-Yuan
authors: CY
authors: Su
authors: Charles C-Y
authors: CC
authors: Shih
authors: Tzuying
authors: T
authors: Chiang
authors: Eugene
authors: E
authors: Chang
authors: YiFen
authors: Y
authors: Lee
authors: Shang Yi
authors: SY
authors: Chiu
authors: Chawnshang
authors: C
authors: Chang
authors: Kuo-Hsiung
authors: KH
authors: Lee
mesh_terms: D000726:Androgen Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006536:Heptanes / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051381:Rats; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: D000726:Androgen Antagonists; D000970:Antineoplastic Agents; D006536:Heptanes