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Content archived on 2024-05-29

Photoactivatable platinum(IV)-diazide complexes: a new generation of platinum-based anticancer agents


The ultimate objective of this research work is the preparation and evaluation of novel photoactive platinum(IV)-diazidecomplexes for combating cancer through their photoactivation selectively at the tumour target site. Platinum(II) drugs are now establish ed as effective anti-tumour agents, the archetypal example of these being cisplatin. However, their usefulness is limited by their narrow spectrum of activity (not active enough against several types of cancer), and by the development of acquired resistance after continuous treatment and toxicity (in particular, nephrotoxicity).

Thus, several third-generation platinum-based drugs have been prepared and tested, a broad class of these concerning platinum(IV) complexes. Platinum(IV) complexes, compared to their platinum(II) analogues, are extremely inert to substitution reactions and are often more lipophilic. Hence, these complexes have enormous potential as anticancer agents in terms of both high activity and low toxicity, but this potential has not been realized by the drugs investigated to date.

This research project is concerned with the synthesis and characterization of new platinum(IV)-diam(m)inediazide derivatives to be evaluated as photoactivatable pro-drugs; in practice, this original approach is intended to facilitate the intra-tumoural activation of platinum(IV)-diam(m)ine derivatives by illumination with visible light to form photolysis products (platinum(II)-diam(m)ine analogues) that irreversibly bind to DNA and are cytotoxic to human cancer cells.

This photoactivation strategy should be generally applicable to platinum(IV)-diazide complexes containing a variety of monodentate amino and chelated diamino ligands. The enormous potential impact of this new class of platinum(IV) photochemotherapeutic agent s relies in their site-specific delivery of a wide range of platinum(II)-diam(m)ine drugs in localized cancers strongly improving their cellular uptake and minimizing unwanted side effects.

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Old College, South Bridge
United Kingdom

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