Issue 6, 2022

Pt(iv) antitumor prodrugs: dogmas, paradigms, and realities

Abstract

Platinum(II)-based drugs are widely used for the treatment of solid tumors, especially in combination protocols. Severe side effects and occurrence of resistance are the major limitations to their clinical use. To overcome these drawbacks, a plethora of Pt(IV) derivatives, acting as anticancer prodrugs, have been designed, synthesized and preclinically (often only in vitro) tested. Here, we summarize the recent progress in the development and understanding of the chemical properties and biochemical features of these Pt(IV) prodrugs, especially those containing bioactive molecules as axial ligands, acting as multi-functional agents. Even though no such prodrugs have been yet approved for clinical use, many show encouraging pharmacological profiles. Thus, a better understanding of their features is a promising approach towards improving the available Pt-based anticancer agents.

Graphical abstract: Pt(iv) antitumor prodrugs: dogmas, paradigms, and realities

Article information

Article type
Perspective
Submitted
16 11 2021
Accepted
24 12 2021
First published
27 12 2021

Dalton Trans., 2022,51, 2121-2134

Pt(IV) antitumor prodrugs: dogmas, paradigms, and realities

M. Ravera, E. Gabano, M. J. McGlinchey and D. Osella, Dalton Trans., 2022, 51, 2121 DOI: 10.1039/D1DT03886A

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