Platinum-based anticancer agents are among the most widely accepted metal-based chemotherapeutics with cisplatin, despite its profound drawbacks, such as severe toxicity, lack of selectivity, inherent and acquired resistance, and transient retention in the bloodstream, still the most clinically and universally used metal-based anticancer agent. Several research efforts have been targeted towards developing alternative platinum-based cytostatic agents that will not only eliminate some of the challenges that are associated with cisplatin but also improve on its cytotoxicity. Most of the synthesized cis-configured complexes, which comprised of mainly the second-generation platinum-based drugs, such as carboplatin, oxaliplatin etc., are yet to be globally accepted and moreover, many of them are still encumbered with some of the limitations that are plaguing the continued use of cisplatin. Among the complexes that are currently being considered by medicinal bioinorganic chemists, platinum(II) complexes with trans-stereochemistry are attract a lot of research interest. This is because the complexes were found to exhibit pharmacodynamics that are relatively complex and radically different from those already established for cisplatin and its derivatives. The initial thought amongst many medicinal bioinorganic researchers that cis-configuration is a prerequisite for cytotoxicity because of the dearth of activity of the non-toxic transplatin, the trans-isomer of cisplatin, has been discarded with recent developments. The dearth of activity of the compound was overcame by replacing and/or modifying the ammine groups with bulky ligands. This article seeks to review some of these trans-platinum compounds and their relevance in anticancer chemotherapy.

From obscurity to prominence: The prospect of trans-platinum compounds in anticancer chemotherapy

ACS Spring 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.