title: Design, synthesis and evaluation of telomerase inhibitory, hTERT repressing, and anti-proliferation activities of symmetrical 1,8-disubstituted amidoanthraquinones.
abstract: A series of symmetrical disubstituded 1,8-diamidoanthraquinones were synthesized and evaluated for anti-proliferation, telomerase inhibitory by TRAP assay, and hTERT expression by SEAP assay. All of the compounds tested, except for compounds 3a and 3s were selected by the NCI screening system. In addition, compounds 4e and 4k exhibited inhibitory effects on telomerase activity. Taken together, our findings indicated that the analysis of cytotoxicity and telomerase inhibition might provide information applicable for further developing potential telomerase targeting strategy.
authors.affiliation: Graduate Institute of Life Sciences, National Defense Medical Center, Taipei 114, Taiwan.
authors.forename: Chia-Chung
authors.initials: CC
authors.lastname: Lee
authors.forename: Kuo-Feng
authors.initials: KF
authors.lastname: Huang
authors.forename: Deh-Ming
authors.initials: DM
authors.lastname: Chang
authors.forename: Jung-Jung
authors.initials: JJ
authors.lastname: Hsu
authors.forename: Fong-Chun
authors.initials: FC
authors.lastname: Huang
authors.forename: Kai-Ning
authors.initials: KN
authors.lastname: Shih
authors.forename: Chun-Liang
authors.initials: CL
authors.lastname: Chen
authors.forename: Tsung-Chih
authors.initials: TC
authors.lastname: Chen
authors.forename: Ruei-Huei
authors.initials: RH
authors.lastname: Chen
authors.forename: Jing-Jer
authors.initials: JJ
authors.lastname: Lin
authors.forename: Hsu-Shan
authors.initials: HS
authors.lastname: Huang
mesh_terms: D000469:Alkaline Phosphatase / Q000378:metabolism; D000880:Anthraquinones / Q000737:chemistry*; D017209:Apoptosis / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*; D019098:Telomerase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D014407:Tumor Cells, Cultured
chemical_list: D000880:Anthraquinones; D004791:Enzyme Inhibitors; C509186:TERT protein, human; D019098:Telomerase; D000469:Alkaline Phosphatase