Biomolecular Interactions of Cytotoxic Ruthenium Compounds with Thiosemicarbazone or Benzothiazole Schiff Base Chelates

Title	Biomolecular Interactions of Cytotoxic Ruthenium Compounds with Thiosemicarbazone or Benzothiazole Schiff Base Chelates
Authors	Dr. Sanam Maikoo, Dr. Bheki Xulu, Dr. Allen Mambanda, Ntando Mkhwanazi, Dr. Candace Davison, Dr. Jo‐Anne de la Mare, Prof. Irvin Noel Booysen
Magazine	Chemmedchem
Date	09/21/2022
DOI	https://doi.org/10.1002/cmdc.202200444
Introduction	This study presents the synthesis and analysis of novel paramagnetic ruthenium compounds, including trans-P-[RuCl(PPh3)2(pmt)]Cl and trans-P-[RuCl(PPh3)2(tmc)]Cl, alongside a diamagnetic ruthenium complex, cis-Cl, trans-P-[RuCl2(PPh3)2(btm)]. These compounds demonstrate dose-dependent binding to genomic DNA and act as DNA intercalators. Furthermore, they inhibit topoisomerase I by nicking supercoiled plasmid DNA. Cytotoxicity assays reveal enhanced activity against cancer cell lines compared to non-tumourigenic controls, with IC50 values in the low micromolar range. Stability studies indicate rapid substitution of chloride co-ligands by nucleophilic species such as DMSO, with significant stability observed in DCM and aqueous phosphate buffer containing DMSO.
Quote	Sanam Maikoo, Bheki A Xulu and Allen Mambanda et al. Biomolecular Interactions of Cytotoxic Ruthenium Compounds with Thiosemicarbazone or Benzothiazole Schiff Base Chelates. ChemMedChem. 2022. DOI: 10.1002/cmdc.202200444

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