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

Jamal El Bakali; Frédérique Klupsch; Aurore Guédin; Bertrand Brassart; Gaëlle Fontaine; Amaury Farce; Pascal Roussel; Raymond Houssin; Jean Luc Bernier; Philippe Chavatte; Jean Louis Mergny; Jean François Riou; Jean Pierre Hénichart

doi:10.1016/j.bmcl.2009.05.025

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

Jamal El Bakali
, Frédérique Klupsch
, Aurore Guédin
, Bertrand Brassart
, Gaëlle Fontaine
, Amaury Farce
, Pascal Roussel
, Raymond Houssin
, Jean Luc Bernier
, Philippe Chavatte
, Jean Louis Mergny
, Jean François Riou
, Jean Pierre Hénichart

Institut de Chimie Pharmaceutique Albert Lespagnol
CNRS
Univ. de Reims Champagne Ardenne
Université de Lille
Ecole Nationale Supérieure de Chimie de Lille

Résultats de recherche: Contribution à un journal › Article › Revue par des pairs

25 Citations (Scopus)

Résumé

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.

langue originale	Anglais
Pages (de - à)	3434-3438
Nombre de pages	5
journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Numéro de publication	13
Les DOIs	https://doi.org/10.1016/j.bmcl.2009.05.025
état	Publié - 1 juil. 2009
Modification externe	Oui

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10.1016/j.bmcl.2009.05.025

Contient cette citation

El Bakali, J., Klupsch, F., Guédin, A., Brassart, B., Fontaine, G., Farce, A., Roussel, P., Houssin, R., Bernier, J. L., Chavatte, P., Mergny, J. L., Riou, J. F., & Hénichart, J. P. (2009). 2,6-Diphenylthiazolo[3,2-b][1,2,4]triazoles as telomeric G-quadruplex stabilizers. Bioorganic and Medicinal Chemistry Letters, 19(13), 3434-3438. https://doi.org/10.1016/j.bmcl.2009.05.025

@article{66a69caef00940abbf6f25f70225a80a,

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.",

keywords = "2,6-Diphenylthiazolo[3,2-b][1,2,4]triazole, Cancer, G-quadruplex, Telomere",

author = "\{El Bakali\}, Jamal and Fr{\'e}d{\'e}rique Klupsch and Aurore Gu{\'e}din and Bertrand Brassart and Ga{\"e}lle Fontaine and Amaury Farce and Pascal Roussel and Raymond Houssin and Bernier, \{Jean Luc\} and Philippe Chavatte and Mergny, \{Jean Louis\} and Riou, \{Jean Fran{\c c}ois\} and H{\'e}nichart, \{Jean Pierre\}",

note = "Funding Information: This work was supported by the {\textquoteleft}Ligue Nationale contre le Cancer, Equipe Labellis{\'e}e 2006{\textquoteright} (to J.F.R.) and EU FP6 {\textquoteleft}MolCancerMed{\textquoteright} LSHC-CT-2004-502943 (to J.L.M.) grants.",

year = "2009",

month = jul,

day = "1",

doi = "10.1016/j.bmcl.2009.05.025",

language = "English",

volume = "19",

pages = "3434--3438",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd",

number = "13",

}

El Bakali, J, Klupsch, F, Guédin, A, Brassart, B, Fontaine, G, Farce, A, Roussel, P, Houssin, R, Bernier, JL, Chavatte, P, Mergny, JL, Riou, JF & Hénichart, JP 2009, '2,6-Diphenylthiazolo[3,2-b][1,2,4]triazoles as telomeric G-quadruplex stabilizers', Bioorganic and Medicinal Chemistry Letters, VOL. 19, Numéro 13, p. 3434-3438. https://doi.org/10.1016/j.bmcl.2009.05.025

TY - JOUR

T1 - 2,6-Diphenylthiazolo[3,2-b][1,2,4]triazoles as telomeric G-quadruplex stabilizers

AU - El Bakali, Jamal

AU - Klupsch, Frédérique

AU - Guédin, Aurore

AU - Brassart, Bertrand

AU - Fontaine, Gaëlle

AU - Farce, Amaury

AU - Roussel, Pascal

AU - Houssin, Raymond

AU - Bernier, Jean Luc

AU - Chavatte, Philippe

AU - Mergny, Jean Louis

AU - Riou, Jean François

AU - Hénichart, Jean Pierre

N1 - Funding Information: This work was supported by the ‘Ligue Nationale contre le Cancer, Equipe Labellisée 2006’ (to J.F.R.) and EU FP6 ‘MolCancerMed’ LSHC-CT-2004-502943 (to J.L.M.) grants.

PY - 2009/7/1

Y1 - 2009/7/1

N2 - 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.

AB - 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.

KW - 2,6-Diphenylthiazolo[3,2-b][1,2,4]triazole

KW - Cancer

KW - G-quadruplex

KW - Telomere

U2 - 10.1016/j.bmcl.2009.05.025

DO - 10.1016/j.bmcl.2009.05.025

M3 - Article

C2 - 19473838

AN - SCOPUS:66749124825

SN - 0960-894X

VL - 19

SP - 3434

EP - 3438

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 13

ER -

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

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