Preclinical Evaluation of Zn(II) Self‐Assemblies with Selective Cytotoxic Activity Against Cancer Cells In Vitro and In Ovo

Dipodal pyridylthiazole amine ligands L1 and L2 both form different metallo‐supramolecular self‐assemblies with Zn2+ and Cu2+ and these are shown to be toxic and selective towards cancer cell lines in vitro. Furthermore, potency and selectivity are highly dependent upon the metal ions, ligand system...

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Published in:Chemistry : a European journal 2024-01, Vol.30 (3), p.e202302803-n/a
Main Authors: Allison, Simon J., Ashton, Gage P., Lynch, Hannah J., Shire, Bethany R., Phillips, Roger M., Parkes, Gareth M. B., Pinder, Emma, Rice, Craig R., Teixeira, Ana A. M., Volleman, Tibo, Wordsworth, Daisy A.
Format: Article
Language:English
Subjects:
Anions
Assemblies
Cancer
Chemistry
Copper
cytotoxic
Cytotoxicity
helicate
Ions
Ligands
Metal ions
Metallography
Metals
Neoplasms
Selectivity
self-assembly
Tumor cell lines
Zinc
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Summary:Dipodal pyridylthiazole amine ligands L1 and L2 both form different metallo‐supramolecular self‐assemblies with Zn2+ and Cu2+ and these are shown to be toxic and selective towards cancer cell lines in vitro. Furthermore, potency and selectivity are highly dependent upon the metal ions, ligand system and bound anion, with significant changes in chemosensitivity and selectivity dependent upon which species are employed. Importantly, significant anti‐tumor activity was observed in ovo at doses that are non‐toxic. Bis‐bidentate ligands L1 and L2 form dinuclear double helicates with Zn2+ and Cu2+ and these self‐assemblies can bind phosphate and 4‐nitrophenylphosphate anions. The complexes show selective cytotoxic and antitumor activity, but this is highly dependent upon which ligand, metal ion and anion are used. The lead compound [(L2)2Zn2]2+ displays in ovo efficacy with a 67 % reduction in tumor weight and 100 % embryo survival rate.
ISSN:0947-6539
1521-3765
DOI:10.1002/chem.202302803