title: Design and synthesis of pironetin analogue/combretastatin A-4 hybrids containing a 1,2,3-triazole ring and evaluation of their cytotoxic activity.
abstract: We here describe the preparation of a series of hybrid molecules containing a combretastatin A-4 moiety and a pironetin analogue fragment connected through a spacer of variable length which includes a 1,2,3-triazole ring. The cytotoxic activities of these compounds have been measured. Relations between structure and cytotoxicity are discussed. Some of the tested compounds showed cytotoxicity values of the same order of magnitude as combretastatin A-4 and were less toxic than the latter compound for normal cells.
authors.affiliation: Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain.
authors.forename: Concepción
authors.initials: C
authors.lastname: Vilanova
authors.affiliation: Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain.
authors.forename: Sandra
authors.initials: S
authors.lastname: Torijano-Gutiérrez
authors.affiliation: Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain.
authors.forename: Santiago
authors.initials: S
authors.lastname: Díaz-Oltra
authors.affiliation: Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain. Electronic address: jmurga@qio.uji.es.
authors.forename: Juan
authors.initials: J
authors.lastname: Murga
authors.affiliation: Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain.
authors.forename: Eva
authors.initials: E
authors.lastname: Falomir
authors.affiliation: Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain.
authors.forename: Miguel
authors.initials: M
authors.lastname: Carda
authors.affiliation: Depart. de Q. Orgánica, Univ. de Valencia, E-46100 Burjassot, Valencia, Spain. Electronic address: alberto.marco@uv.es.
authors.forename: J
authors.initials: J
authors.lastname: Alberto Marco
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000494:pharmacology*; D001632:Bibenzyls / Q000737:chemistry*; D049109:Cell Proliferation / Q000187:drug effects*; D002478:Cells, Cultured; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005434:Flow Cytometry; D057809:HEK293 Cells; D006801:Humans; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D011753:Pyrones / Q000737:chemistry*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D001632:Bibenzyls; D011753:Pyrones; D014230:Triazoles; C088446:pironetin; C040105:combretastatin
keywords: Click reaction; Combretastatin A-4; Cytotoxicity; Hybrid molecules; Pironetin analogues; Tubulin-active compounds