2,6-Diphenylthiazolo[3,2-b][1,2,4]triazoles as telomeric G-quadruplex stabilizers

被引：20

作者：

El Bakali, Jamal ^{[2
]}

Klupsch, Frederique ^{[2
]}

Guedin, Aurore ^{[1
]}

Brassart, Bertrand ^{[3
]}

Fontaine, Gaelle ^{[4
]}

Farce, Amaury ^{[5
]}

Roussel, Pascal ^{[6
]}

Houssin, Raymond ^{[2
]}

Bernier, Jean-Luc ^{[4
]}

Chavatte, Philippe ^{[5
]}

Mergny, Jean-Louis ^{[1
]}

Riou, Jean-Francois ^{[1
]}

Henichart, Jean-Pierre ^{[2
]}

机构：

[1] CNRS, INSERM, U565, Museum Natl Hist Nat,UMR 7196,USM 503, F-75005 Paris, France

[2] Univ Lille 2, Inst Chim Pharmaceut Albert Lespagnol, EA 2692, IFR 114, F-59006 Lille, France

[3] Univ Reims, JE 2428, Lab Oncopharmacol, F-51096 Reims, France

[4] Univ Sci & Technol Lille, CNRS, UMR 8009, Chim Organ Phys Lab, F-59655 Villeneuve Dascq, France

[5] Univ Lille 2, Chim Therapeut Lab, Fac Pharm, EA 1643,IFR 114, F-59006 Lille, France

[6] ENSCL, Unite Catalyse & Chim Solide, CNRS, UMR 8181, F-59652 Villeneuve Dascq, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 13期

关键词：

G-quadruplex; Telomere; Cancer; 2,6-Diphenylthiazolo[3,2-b][1,2,4]triazole; CLICK CHEMISTRY; HUMAN FIBROBLASTS; LIGANDS; DNA; DERIVATIVES; INHIBITION; COMPOUND; SCAFFOLD; BINDING; CELLS;

D O I：

10.1016/j.bmcl.2009.05.025

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：3434 / 3438

页数：5

共 28 条

[1] TELOMERE LENGTH PREDICTS REPLICATIVE CAPACITY OF HUMAN FIBROBLASTS [J].