Water-soluble copper pyrithione complexes with cytotoxic and antibacterial activity

  • Org Biomol Chem. 2023 Mar 22;21(12):2539-2544. doi: 10.1039/d2ob01224c.
Atreyee Mishra  1 ,  Karrera Y Djoko  2 ,  Yi-Hsuan Lee  3 ,  Rianne M Lord  3 ,  Grace Kaul  4  5 ,  Abdul Akhir  4 ,  Deepanshi Saxena  4 ,  Sidharth Chopra  4  5 ,  James W Walton  1
Affiliations
  • 1. Durham University, Department of Chemistry, Lower Mountjoy, Durham, DH1 3LE, UK. [email protected].
  • 2. Durham University, Department of Biosciences, Upper Mountjoy, Durham, DH1 3LE, UK.
  • 3. School of Chemistry, University of East Anglia, Norwich Research Park, Norwich, Norfolk, NR4 7TJ, UK.
  • 4. Division of Molecular Microbiology and Immunology, CSIR-Central Drug Research Institute, Sitapur Road, Sector 10, Janakipuram Extension, Lucknow-226031, Uttar Pradesh, India.
  • 5. Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India.
PMID: 36877005 DOI: 10.1039/d2ob01224c
Abstract

Copper Pyrithione, [Cu(PyS)2] has shown excellent biological activity against Cancer cells and Bacterial cells, however, it has extremely low aqueous solubility, limiting its applicability. Herein, we report a series of PEG-substituted pyrithione copper(II) complexes with significantly increased aqueous solubility. While long PEG chains lead to a decrease in bioactivity, the addition of short PEG chains leads to improved aqueous solubility with retention of activity. One novel complex, [Cu(PyS1)2], has particularly impressive Anticancer activity, surpassing that of the parent complex.

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