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Updated: Jan 6, 2026
Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
Therapeutic Potential of 2,2':6',2″-Terpyridine-Based Au(III), Pt(II), and Mn(II) Complexes against 2D and 3D Human
Katarzyna Choroba1, Barbara Machura1, Mateusz Penkala1
1Institute of Chemistry, University of Silesia, Szkolna 9, 40-006 Katowice, Poland.
Abstract:
The antiproliferative effect of [AuCl(tmp-terpy)](PF6)2 (1), [PtCl(tmp-terpy)](CF3SO3) (2), [MnCl2(tmp-terpy)] (3), and 4'-(3,4,5-trimethoxy-phenyl)-2,2':6',2″-terpyridine (tmp-terpy) was analyzed in sensitive and doxorubicin-resistant (DoxR) colorectal cancer (CRC) cell lines and in normal primary human fibroblasts. Comprehensive studies were performed for 1 and tmp-terpy, showing the strongest cytotoxicity in HCT116DoxR 2D cells and having the capability to induce the loss of cell viability in 3D HCT116DoxR spheroids. Complex 1 internalizes CRC-resistant cancer cells and increases the number of reactive oxygen species (ROS), triggering cell death by apoptosis and autophagy. Changes in protein expression levels of HCT116DoxR cells exposed to 1 and tmp-terpy primarily affect protein folding, apoptosis, and stress response, consistent with the observed induction of programmed cell death and ROS. The combination of 1 or tmp-terpy with oxaliplatin (OX) and cisplatin (Cis) shows cytotoxic effects in 3D CRC-resistant spheroids. No in vivo toxicity in a chicken embryo is observed, even when 1 is combined with an OX and Cis.
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