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Synthesis and anti-cancer activity of bis-amino-phosphine ligand and its ruthenium(II) complexes.

Authors
  • Engelbrecht, Zelinda1
  • Roberts, Kim Elli1
  • Hussan, Ayesha2
  • Amenuvor, Gershon3
  • Cronjé, Marianne Jaqueline4
  • Darkwa, James5
  • Makhubela, Banothile C E5
  • Sitole, Lungile6
  • 1 Department of Biochemistry, University of Johannesburg, PO Box 524, Auckland Park, Johannesburg 2006, South Africa; School of Molecular and Cell Biology, University of the Witwatersrand, Private Bag 3, Wits 2050, South Africa. , (South Africa)
  • 2 Department of Biochemistry, University of Johannesburg, PO Box 524, Auckland Park, Johannesburg 2006, South Africa. , (South Africa)
  • 3 Research Centre for Synthesis and Catalysis, Department of Chemical Sciences, University of Johannesburg, Auckland Park, Johannesburg 2006, South Africa; Council for Scientific and Industrial Research (CSIR) Institute of Industrial Research, PO Box LG 576, Accra, Ghana. , (Ghana)
  • 4 School of Molecular and Cell Biology, University of the Witwatersrand, Private Bag 3, Wits 2050, South Africa. , (South Africa)
  • 5 Research Centre for Synthesis and Catalysis, Department of Chemical Sciences, University of Johannesburg, Auckland Park, Johannesburg 2006, South Africa. , (South Africa)
  • 6 Department of Biochemistry, University of Johannesburg, PO Box 524, Auckland Park, Johannesburg 2006, South Africa. Electronic address: [email protected] , (South Africa)
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Aug 11, 2020
Volume
30
Issue
20
Pages
127492–127492
Identifiers
DOI: 10.1016/j.bmcl.2020.127492
PMID: 32791194
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

The development of both chemotherapeutic drug resistance as well as adverse side effects suggest that the current chemotherapeutic drugs remain ineffective in treating the various types of cancers. The development of new metallodrugs presenting anti-cancer activity is therefore needed. Ruthenium complexes have gained a great deal of interest due to their promising anti-tumour properties and reduced toxicity in vivo. This study highlighted the effective induction of cell death in a malignant melanoma cell by two novel bis-amino-phosphine ruthenium(II) complexes referred to as GA105 and GA113. The IC50 concentrations were determined for both the complexes, the ligand and cisplatin, for comparison. Both complexes GA105 and GA113 displayed a high anti-cancer selectivity profile as they exhibited low IC50 values of 6.72 µM and 8.76 µM respectively, with low toxicity towards a non-malignant human cell line. The IC50 values obtained for both complexes were lower than that of cisplatin. The new complexes were more effective compared to the free ligand, GA103 (IC50 = >20 µM). Morphological studies on treated cells induced apoptotic features, which with further studies could indicate an intrinsic cell death pathway. Additionally, flow cytometric analysis revealed that the mode of cell death of complex GA113 was apoptosis. The outcomes herein give further insight into the potential use of selected Ru(II) complexes as alternative chemotherapeutic drugs in the future. Copyright © 2020 Elsevier Ltd. All rights reserved.

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