title: Synthesis and biological evaluation of 3-(4-fluorophenyl)-1H-pyrazole derivatives as androgen receptor antagonists.
abstract: A novel series of 3-(4-fluorophenyl)-1H-pyrazole derivatives were synthesized and evaluated for their antiproliferative activity against two prostate cancer cell lines (LNCaP and PC-3) and androgen receptor target gene prostate-specific antigen (PSA) inhibitory activity in LNCaP cells. Several compounds showed potent antiproliferative activity against LNCaP cells and showed a promising PSA downregulation rate. Among these, compound 10e selectively inhibited LNCaP cell growth with an IC50 value of 18 μmol/l and showed a PSA downregulation rate of 46%, which was better than the lead compound T3.
authors.affiliation: Key Laboratory of Chemical Biology, Ministry of Education, Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan, People's Republic of China.
authors.forename: Guangzhu
authors.initials: G
authors.lastname: Guo
authors.forename: Jianzhen
authors.initials: J
authors.lastname: Liu
authors.forename: Guanjie
authors.initials: G
authors.lastname: Wang
authors.forename: Daoguang
authors.initials: D
authors.lastname: Zhang
authors.forename: Jinjie
authors.initials: J
authors.lastname: Lu
authors.forename: Guisen
authors.initials: G
authors.lastname: Zhao
mesh_terms: D000814:Aniline Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D015536:Down-Regulation; D006801:Humans; D008297:Male; D017430:Prostate-Specific Antigen / Q000037:antagonists & inhibitors / Q000378:metabolism; D011471:Prostatic Neoplasms; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: C000608799:4-fluoro-N-((3-(4-fluorophenyl)-1-methyl-1H-pyrazole-5-yl)methyl)aniline; D000814:Aniline Compounds; D000970:Antineoplastic Agents; D001549:Benzamides; D011720:Pyrazoles; D017430:Prostate-Specific Antigen