Literature DB >> 19473838

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

Jamal El Bakali1, 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.   

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.

Entities:  

Mesh:

Substances:

Year:  2009        PMID: 19473838     DOI: 10.1016/j.bmcl.2009.05.025

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Anticancer activity and cellular repression of c-MYC by the G-quadruplex-stabilizing 11-piperazinylquindoline is not dependent on direct targeting of the G-quadruplex in the c-MYC promoter.

Authors:  Peda V L Boddupally; Seongmin Hahn; Cristina Beman; Biswanath De; Tracy A Brooks; Vijay Gokhale; Laurence H Hurley
Journal:  J Med Chem       Date:  2012-06-25       Impact factor: 7.446

2.  Interaction of pyrrolobenzodiazepine (PBD) ligands with parallel intermolecular G-quadruplex complex using spectroscopy and ESI-MS.

Authors:  Gajjela Raju; Ragampeta Srinivas; Vangala Santhosh Reddy; Mohammed M Idris; Ahmed Kamal; Narayana Nagesh
Journal:  PLoS One       Date:  2012-04-27       Impact factor: 3.240

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.