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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Computer Simulation
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Crystallography, X-Ray
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Drug Design
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Fluorescence Resonance Energy Transfer
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G-Quadruplexes / drug effects*
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Telomere / chemistry*
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Telomere / metabolism
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Thiazoles / chemical synthesis*
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Thiazoles / chemistry
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Thiazoles / pharmacology
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Transition Temperature
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Triazoles / chemical synthesis*
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Triazoles / chemistry
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Triazoles / pharmacology
Substances
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2,6-diphenylthiazolo(3,2-b)(1,2,4)triazole
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Thiazoles
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Triazoles