Synthesis and telomeric G-quadruplex-stabilizing ability of macrocyclic hexaoxazoles bearing three side chains

Synthesis and telomeric G-quadruplex-stabilizing ability of macrocyclic hexaoxazoles bearing three side chains

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...

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Bibliographic Details
Main Authors: Ma, Yue, Iida, Keisuke, Sasaki, Shogo, Hirokawa, Takatsugu, Heddi, Brahim, Nagasawa, Kazuo, Phan, Anh Tuân
Other Authors: School of Physical and Mathematical Sciences
Format: Article
Language:English
Published: 2019
Subjects:
DRNTU::Science::Physics
G-Quadruplex
Macrocyclic Oxazole
Online Access:https://hdl.handle.net/10356/105834
http://hdl.handle.net/10220/48766
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Institution: Nanyang Technological University
Language: English
Description
Summary: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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