title: 2,6-Diphenylthiazolo[3,2-b][1,2,4]triazoles as telomeric G-quadruplex stabilizers.
abstract: The design and synthesis of 2,6-diphenylthiazolo[3,2-b][1,2,4]triazoles characterized by a large aromatic building block bearing cationic side chains are reported. These molecules are evaluated as telomeric G-quadruplex stabilizers and for their selectivity towards duplex DNA by competition experiments. Two compounds (14a, 19) were found active with high selectivity for telomeric G-quadruplex over duplex DNA.
authors.affiliation: Institut de Chimie Pharmaceutique Albert Lespagnol, EA 2692, IFR 114, Université de Lille 2, 3 rue du Professeur Laguesse, BP 83, 59006 Lille, France.
authors.forename: Jamal
authors.initials: J
authors.lastname: El Bakali
authors.forename: Frédérique
authors.initials: F
authors.lastname: Klupsch
authors.forename: Aurore
authors.initials: A
authors.lastname: Guédin
authors.forename: Bertrand
authors.initials: B
authors.lastname: Brassart
authors.forename: Gaëlle
authors.initials: G
authors.lastname: Fontaine
authors.forename: Amaury
authors.initials: A
authors.lastname: Farce
authors.forename: Pascal
authors.initials: P
authors.lastname: Roussel
authors.forename: Raymond
authors.initials: R
authors.lastname: Houssin
authors.forename: Jean-Luc
authors.initials: JL
authors.lastname: Bernier
authors.forename: Philippe
authors.initials: P
authors.lastname: Chavatte
authors.forename: Jean-Louis
authors.initials: JL
authors.lastname: Mergny
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Riou
authors.forename: Jean-Pierre
authors.initials: JP
authors.lastname: Hénichart
mesh_terms: D003198:Computer Simulation; D018360:Crystallography, X-Ray; D015195:Drug Design; D031541:Fluorescence Resonance Energy Transfer; D054856:G-Quadruplexes / Q000187:drug effects*; D016615:Telomere / Q000737:chemistry* / Q000378:metabolism; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D044366:Transition Temperature; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: C542855:2,6-diphenylthiazolo(3,2-b)(1,2,4)triazole; D013844:Thiazoles; D014230:Triazoles