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Related Experiment Video

Updated: Feb 15, 2026

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents

Published on: May 28, 2014

Dual functional dinuclear platinum complex with selective reactivity towards c-myc G-quadruplex.

Lei He¹, Zhenyu Meng¹, Dechen Xu¹

¹Division of Chemistry and Biological Chemistry, School of Physical and Mathematical Sciences, Nanyang Technological University, 21 Nanyang Link, Singapore, 637371, Singapore.

Scientific Reports

|January 17, 2018

Summary

Researchers developed novel dinuclear platinum complexes for targeting G-quadruplexes (GQ). These complexes offer a covalent strategy for anticancer drug development by binding to oncogenic G-rich sequences.

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Last Updated: Feb 15, 2026

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The Synthesis, Characterization and Reactivity of a Series of Ruthenium N-triphosPh Complexes

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Published on: April 10, 2015

Area of Science:

Medicinal Chemistry
Supramolecular Chemistry
Oncology

Background:

G-quadruplexes (GQ) are promising anticancer targets due to their role in oncogenic G-rich sequences.
Current therapeutic strategies primarily use non-covalent binders, leaving covalent targeting underexplored.

Purpose of the Study:

To design and synthesize novel dinuclear platinum complexes for covalent targeting of G-quadruplexes.
To investigate the dual-functional binding mechanism of these complexes to G-quadruplex structures.

Main Methods:

Synthesis of dinuclear platinum complexes with varying alkyl linkages.
Characterization of platinum complexes and their binding interactions with G-quadruplexes.
Evaluation of the specificity towards c-myc G-quadruplex.

Main Results:

A series of dinuclear platinum complexes, specifically Pt3 with a nonanediamine linkage, demonstrated optimized binding to the c-myc G-quadruplex.
The complexes exhibit a dual-functional binding mode: non-covalent π-stacking by aromatic ligands and covalent chelation by Pt(II) cores.
Covalent chelation occurred at both 3'- and 5'-ends of the guanines within the G-quadruplex structure.

Conclusions:

Dinuclear platinum complexes represent a novel covalent strategy for targeting G-quadruplexes.
The designed complexes show potential as anticancer therapeutics by specifically binding and stabilizing oncogenic G-quadruplex structures.