Water-soluble copper pyrithione complexes with cytotoxic and antibacterial activity.

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.