Substitution Kinetics, DNA/BSA Interactions, Cytotoxicity Evaluation and Computational Analysis of [bis‐(azaaryl)amine)Pt(II)/Pd(II)Cl] Complexes, Azaaryl = Quinoline or Phenanthridine
Phakamani C. Dlamini, Thato T. Medupe, Lucy W. Macharia, Karabo Serala, Sharon Prince, Gregory S. Smith, Irvin N. Booysen, Allen Mambanda
TL;DR
This study explores new platinum and palladium complexes as potential anticancer drugs, showing promising interactions with DNA and proteins, and better efficacy than cisplatin in some cancer cell lines.
Contribution
The paper introduces novel bis(azaaryl)amine Pt(II)/Pd(II)Cl complexes with improved DNA/BSA interactions and cytotoxicity profiles.
Findings
Pt/Pd complexes showed strong DNA and BSA binding with potential as groove binders and partial intercalators.
PtL1Cl demonstrated superior efficacy against breast and pancreatic cancer cells compared to cisplatin.
Molecular docking predicted strong binding affinity to protease-inhibiting proteins linked to cancer progression.
Abstract
The search for metal‐based anticancer agents with improved efficacy and reduced side effects is ongoing. The activities of these anticancer drugs depend on their aqueous stability, substitutional reactivity at target sites (cytotoxicity) and nontarget sites (toxicity), as well as their transportation and cell bioavailability. In this study, six square‐planar Pt(II) and Pd(II) complexes (Pt/PdL1Cl‐3), all bearing the bis(azaaryl)amine (azaaryl = quinoline or phenanthridine) chelating ligands, were synthesised and characterised by various spectroscopic methods. Their biochemical interactions with bovine serum albumin (BSA)/deoxyribonucleic acid (DNA) and rates of ligand exchange with biological nucleophiles (guanine and thiourea) were probed spectrophotometrically. DFT‐optimised molecular structures in Gaussian 9 were computed. Molecular docking simulations of the optimised structures at…
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Taxonomy
TopicsMetal complexes synthesis and properties · Ferrocene Chemistry and Applications · Synthesis of Tetrazole Derivatives