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Updated: Jan 8, 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
Additional functionality for plecstatin-1-analogous anticancer Ru(η6-p-cymene)Cl complexes
Shahid Iqbal1, Adnan Ashraf2, Anne Dill3
1School of Chemical Sciences, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand; Institute of Chemistry, University of Sargodha, Sargodha 40100, Pakistan.
Abstract:
The bioactivity of organometallic compounds can be enhanced by modifying the ligand to achieve higher potency or an altered mode of action. Here, we conjugated amino acids to pyridine-2-carbothioamides (PCAs) and formed their RuII(cym)Cl (cym = η6-p-cymene) organometallics, as confirmed by mass spectrometry, NMR spectroscopy and elemental analysis. The in vitro antiproliferative activities of ligands 1-4 and complexes 1a-4a were established against human non-small cell lung carcinoma (NCI-H460), cervical carcinoma (SiHA), colorectal carcinoma (HCT116) and colon adenocarcinoma (SW480) cell lines. Complexes 1a-3a showed no activity but 4a was moderately potent with an IC50 value of 35 μM in NCI-H460 cells. Organoruthenium compound 4a was also more active than its PCA ligand 4 and the clinically investigated Ru complex KP1339 in NCI-H460 cells.
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