2,6-Diphenylthiazolo[3,2-b][1,2,4]triazoles as telomeric G-quadruplex stabilizers.
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.
El Bakali
Jamal
J
Institut de Chimie Pharmaceutique Albert Lespagnol, EA 2692, IFR 114, Université de Lille 2, 3 rue du Professeur Laguesse, BP 83, 59006 Lille, France.
Klupsch
Frédérique
F
Guédin
Aurore
A
Brassart
Bertrand
B
Fontaine
Gaëlle
G
Farce
Amaury
A
Roussel
Pascal
P
Houssin
Raymond
R
Bernier
Jean-Luc
JL
Chavatte
Philippe
P
Mergny
Jean-Louis
JL
Riou
Jean-François
JF
Hénichart
Jean-Pierre
JP
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
C542855:2,6-diphenylthiazolo(3,2-b)(1,2,4)triazole; D013844:Thiazoles; D014230:Triazoles