Issue 33, 2016

Platinum(iv) anticancer prodrugs – hypotheses and facts

Abstract

In this manuscript we focus on Pt(IV) anticancer prodrugs. We explore the main working hypotheses for the design of effective Pt(IV) prodrugs and note the exceptions to the common assumptions that are prevalent in the field. Special attention was devoted to the emerging class of “dual action” Pt(IV) prodrugs, where bioactive ligands are conjugated to the axial positions of platinum in order to obtain orthogonal or complementary effects that will increase the efficacy of killing the cancer cells. We discuss the rationale behind the design of the “dual action” prodrugs and the results of the pharmacological studies obtained. Simultaneous release of two bioactive moieties inside the cancer cells often triggers several processes that together determine the fate of the cell. Pt(IV) complexes provide many opportunities for applying new concepts in targeting, synergistic cell killing and exploiting novel nanodelivery systems.

Graphical abstract: Platinum(iv) anticancer prodrugs – hypotheses and facts

Article information

Article type
Perspective
Submitted
12 Apr 2016
Accepted
16 May 2016
First published
23 May 2016

Dalton Trans., 2016,45, 12983-12991

Platinum(IV) anticancer prodrugs – hypotheses and facts

D. Gibson, Dalton Trans., 2016, 45, 12983 DOI: 10.1039/C6DT01414C

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