Metabolite

Biotechnology

Biology

Pharmacokinetics

Prodrug

Active metabolite

Biochemistry

Stereochemistry

In vivo

In vitro

Internal medicine

Cytotoxic T cell

Pharmacology

Chemotherapy

Medicine

Chemistry

Lipophilicity

International Journal of Molecular Sciences

A chemo-anti-inflammatory strategy is of interest for the treatment of aggressive cancers. The platinum (IV) prodrug with non-steroidal anti-inflammatory drugs (NSAIDs) as axial ligands is designed to efficiently enter tumor cells due to high lipophilicity and release the cytotoxic metabolite and NSAID intracellularly, thereby reducing side effects and increasing the therapeutic efficacy of platinum chemotherapy. Over the last 7 years, a number of publications have been devoted to the design of such Pt(IV) prodrugs in combination with anti-inflammatory chemotherapy, with high therapeutic efficacy in vitro and In vivo. In this review, we summarize the studies devoted to the development of Pt(IV) prodrugs with NSAIDs as axial ligands, the study of the mechanism of their cytotoxic action and anti-inflammatory activity, the structure–activity ratio, and therapeutic efficacy.

Pt(IV) Prodrugs with NSAIDs as Axial Ligands