Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 13, Pages 3434-3438Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.05.025
Keywords
G-quadruplex; Telomere; Cancer; 2,6-Diphenylthiazolo[3,2-b][1,2,4]triazole
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Funding
- 'Ligue Nationale contre le Cancer, Equipe Labellisee
- EU FP6 'MolCancerMed' [LSHC-CT-2004-502943]
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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.
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