Article Dans Une Revue Molecules Année : 2019

Synthesis and Telomeric G-Quadruplex-Stabilizing Ability of Macrocyclic Hexaoxazoles Bearing Three Side Chains

Résumé

G-quadruplexes (G4s), which are structures formed in guanine-rich regions of DNA, are involved in a variety of significant biological functions, and therefore “sequence-dependent” selective G4-stabilizing agents are required as tools to investigate and modulate these functions. Here, we describe the synthesis of a new series of macrocyclic hexaoxazole-type G4 ligand (6OTD) bearing three side chains. One of these ligands, 5b, stabilizes telomeric G4 preferentially over the G4-forming DNA sequences of c-kit and K-ras, due to the interaction of its piperazinylalkyl side chain with the groove of telomeric G4.

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hal-02370067 , version 1 (29-07-2025)

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Yue Ma, Keisuke Iida, Shogo Sasaki, Takatsugu Hirokawa, Brahim Heddi, et al.. Synthesis and Telomeric G-Quadruplex-Stabilizing Ability of Macrocyclic Hexaoxazoles Bearing Three Side Chains. Molecules, 2019, 24 (2), pp.263. ⟨10.3390/molecules24020263⟩. ⟨hal-02370067⟩
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