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Exploring new strategies for the development of platinum(IV) anticancer drugs

Recently published paper in Angewandte Chemie explores equatorial substitutions in platinum(IV) complexes.

We are thrilled to highlight a recent joint publication of Alexander Kastner and Hemma Schueffl from the group of Prof. Christian Kowol from the Institute of Inorganic Chemistry, University of Vienna and Prof. Petra Heffeter from the Center for Cancer Research, Medical University of Vienna.

Typically, platinum(IV) anticancer drugs have to be synthesized from the respective platinum(II) precursors. Herein, we developed a method to exchange the equatorial ligands of intact platinum(IV) complexes, enabling the synthesis of otherwise inaccessible derivatives. We could show that introduction of an albumin-binding, tumor-targeting maleimide moiety at this position resulted in strongly increased antitumor activity. This novel synthesis strategy offers the possibility to design targeted triple-action platinum(IV) prodrugs, with an equatorial maleimide moiety and two different bioactive compounds in axial position.

The full paper is available open access at Angewandte Chemie: