56041-59-9Relevant academic research and scientific papers
Antitumor agents 222. Synthesis and anti-androgen activity of new diarylheptanoids
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
, p. 5083 - 5090 (2003)
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 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.
