title: Synthesis, cytotoxic effects and tubulin polymerization inhibition of 1,4-disubstituted 1,2,3-triazole analogs of 2-methoxyestradiol.
abstract: Thirteen 1,4-disubstituted 1,2,3-triazole analogs of 2-methoxyestradiol were prepared and tested for their cytotoxic and tubulin polymerization inhibition effects. Two compounds, 11j and 11k, exhibited anti-proliferative effects at low micromolar concentrations. The two analogs 11j and 11k also inhibited tubulin assembly with IC50 values of 8.1 and 5.9μM, respectively.
authors.affiliation: School of Pharmacy, Department of Pharmaceutical Chemistry, University of Oslo, PO Box 1068, Blindern, N-0316 Oslo, Norway.
authors.forename: Eirik Johansson
authors.initials: EJ
authors.lastname: Solum
authors.affiliation: School of Pharmacy, Department of Pharmaceutical Chemistry, University of Oslo, PO Box 1068, Blindern, N-0316 Oslo, Norway.
authors.forename: Anders
authors.initials: A
authors.lastname: Vik
authors.affiliation: School of Pharmacy, Department of Pharmaceutical Chemistry, University of Oslo, PO Box 1068, Blindern, N-0316 Oslo, Norway. Electronic address: t.v.hansen@farmasi.uio.no.
authors.forename: Trond Vidar
authors.initials: TV
authors.lastname: Hansen
mesh_terms: D000077584:2-Methoxyestradiol; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D060326:Chemistry Techniques, Synthetic; D004958:Estradiol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D020014:K562 Cells; D055503:Protein Multimerization / Q000187:drug effects*; D020836:Protein Structure, Quaternary; D014230:Triazoles / Q000737:chemistry*; D014404:Tubulin / Q000737:chemistry*; D050257:Tubulin Modulators / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D014230:Triazoles; D014404:Tubulin; D050257:Tubulin Modulators; D004958:Estradiol; D000077584:2-Methoxyestradiol
keywords: 1,2,3-Triazoles; 2-Methoxyestradiol; Anti-cancer; Cytotoxicity; Estrogens; Tubulin inhibition