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Insertion of (Bioactive) Equatorial Ligands into Platinum(IV) Complexes by Alexander Kastner; Hemma Schueffl; Patrick A. Yassemipour; Bernhard K. Keppler; Petra Heffeter; Christian R. Kowol is a Chemistry article available to read on EtoBox.

What is Insertion of (Bioactive) Equatorial Ligands into Platinum(IV) Complexes about?

## Abstract Platinum(IV) prodrugs are highly interesting alternatives to platinum(II) anticancer therapeutics due to their increased tumor selectivity and reduced side effects. In contrast to the established theory, we recently observed that the equatorial ligand(s) of e.g. oxaliplatin(IV) complexes can be hydrolyzed with formation of [(DACH)Pt(OH~eq~)~2~(OAc~ax~)~2~]. In the work presented here, we investigated the reactivity and synthetic usability of this complex to be exploited as a precursor for the development of novel platinum(IV) complexes, not able to be synthesized by conventional protocols. Indeed, we could substitute the equatorial hydroxido ligand(s) e.g. by one or two monodentate biotin ligands (which would be oxidized under standard methods). The formed complexes turned out to be very stable with slow ligand release after reduction, ideal for long‐circulating tumor‐targeting strategies. Therefore, two platinum(IV) complexes with equatorial maleimides, capable of exploiting serum albumin as a natural nanocarrier, were synthesized as well. The complexes showed massively prolonged plasma half‐life and distinctly improved anticancer activity in vivo compared to oxaliplat

Who reads Insertion of (Bioactive) Equatorial Ligands into Platinum(IV) Complexes?

Author

Alexander Kastner; Hemma Schueffl; Patrick A. Yassemipour; Bernhard K. Keppler; Petra Heffeter; Christian R. Kowol

Publisher

John Wiley and Sons Inc.

Published

2023

Language

EN

Field

Chemistry (Physical Sciences)