4.5 Article

Anticancer evaluation of ruthenium(III) complexes with N-donor ligands tethered to coumarin or uracil moieties

Journal

INORGANICA CHIMICA ACTA
Volume 492, Issue -, Pages 98-107

Publisher

ELSEVIER SCIENCE SA
DOI: 10.1016/j.ica.2019.04.018

Keywords

Ruthenium; Dipicolyamine; Chromone; Uracil; DNA interactions; Cytotoxicity

Funding

  1. South African Research Chairs Initiative of the Department of Science and Technology (DST) [98566]
  2. National Research Foundation of South Africa (NRF) [98566]
  3. NRF CPRR [105829]
  4. Thuthuka NRF [94020]
  5. Incentive Funding for Rated Researchers NRF [114737]
  6. Rhodes University
  7. University of KwaZulu-Natal

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In this study, the synthesis and characterization of new paramagnetic ruthenium(III) complexes: cis-[RuCl2(urdpa)] (1) {Hurdpa = 6-((bis(pyridin-2-ylmethyl)amino)methyl)uracil} and fac-[RuCl3(chrdpa)] (2) {chrdpa = 4-((bis(pyridin-2-ylmethyl)amino)methyl)-7-methoxycoumarin} are reported. These metal complexes have been comprehensively characterized by an array of physicochemical techniques and the X-ray solid-state structures of 1 and Hurdpa have been attained. Electronic spectroscopy Calf-Thymus DNA titrations revealed that both 1 and 2 are groove binders while molecular docking calculations indicated that the ligands' steric factors dictate the mode of interaction of these individual ruthenium(III) species. These mononuclear ruthenium compounds were screened against cervical and breast cancer cell lines and show activity in the high micromolar range.

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