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Updated: Mar 26, 2026

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies
Published on: February 17, 2023
Unique Use of Alkylation for Chemo-Redox Activity by a Pt(IV) Prodrug
Rakesh K Pathak1, Shanta Dhar2
1NanoTherapeutics Research Laboratory, Department of Chemistry, University of Georgia, Athens, GA, 30602, USA), Fax: (+1) 706-542-9454.
Abstract:
Resistance towards chemotherapeutics displayed by cancer cells is a significant stumbling block against fruitful cisplatin-based therapy. A unique dual-acting chemotherapeutic modality, Platin-B, a prodrug of cisplatin and pipobroman-mimicking alkylating agent, was constructed to circumvent tumor resistance. Platin-B exhibited a superior cytotoxicity profile in cisplatin-resistant cancer cells. Enhanced activity and the ability to overcome cancer-induced resistance of Platin-B was related to adduct formation with intracellular glutathione, followed by the activity of Platin-B on the mitochondria of cells, along with its conventional nuclear activity. Alkylating moieties present on Platin-B enhanced its cellular and subcellular concentration and protected it from early drug sequestration by biological thiols.
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