Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 18, Issue 31, Pages 6147-6154Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d0ob00983k
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Funding
- Russian Science Foundation [18-74-00051, 20-15-00017, 19-75-10109, 075-15-2019-1669]
- Ministry of Science and Higher Education of the Russian Federation
- Russian Science Foundation [18-74-00051, 20-15-00017, 19-75-10109] Funding Source: Russian Science Foundation
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G-quadruplexes (G4) represent one class of non-canonical secondary nucleic acid structures that are currently regarded as promising and attractive targets for anti-cancer, anti-viral and antibacterial therapy. Herein, we probe a new i-clamp-inspired phenoxazine scaffold for designing G4-stabilizing ligands. The length of the protonated aminoalkyl tethers ('arms') of the phenoxazine-based ligand was optimizedin silico. Two double-armed ligands differing in the relative orientation of their arms and one single-armed ligand were synthesized. The two-armed ligands significantly enhanced the thermal stability of the G-quadruplex structures (increasing the melting temperature by up to 20 degrees C) and displayed G4 selectivity over duplex DNA. The ligands look promising for biological studies and the phenoxazine scaffold could be a starting point for designing new G4-interacting compounds.
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