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Pt-TEMPO

Development stage: Preclinical
Modality: Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules

Overview

Pt-TEMPO is a spin-labelled photoactivatable platinum(IV) prodrug designed as an anticancer complex. It exhibits low toxicity in the dark but becomes highly active upon irradiation with blue visible light. Photoactivation leads to the release of Pt(II), azidyl radicals, and nitroxyl radicals. This mechanism enables its potent activity against human ovarian cancer cells, demonstrating efficacy comparable to the clinical photosensitizer chlorpromazine and superior activity to the anticancer drug cisplatin under the tested conditions. [cite: PMID: 27189101]

Other names: trans,trans,trans-[Pt(N3)2(OH)(OCOCH2CH2CONH-TEMPO)(Py)2]

Targets

DNA

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