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© 2021 American Chemical Society.Terpyridine platinum (TP)–based chemotherapeutic agents target three–dimensional structures on DNA known as G–quadruplexes. We report the rational design and synthesis of a TP conjugate combined with copper–64 (64Cu), the decay characteristics of which include emission of β– and Auger electrons for radiotherapy and β+ particles for positron emission tomography (PET) imaging. The present experimental studies show that the novel [64Cu]Cu–1,4,7–triazacyclononane–1,4,7–triacetic acid (NOTA)–TP is stable, permitting selective killing of cancer cells. The antitumor activity of [64Cu]Cu–NOTA–TP at high apparent molar activity is in the low nanomolar range and 27,800–fold greater than that of natCu–NOTA–TP at 24 h post treatment. These results suggest that this combination of a cytotoxic TP agent with 64Cu has considerable potential for cancer treatment and PET imaging.
