Title:Recent Progresses in Conjugation with Bioactive Ligands to Improve
the Anticancer Activity of Platinum Compounds
Volume: 29
Issue: 15
Author(s): Marco Zuccolo, Noemi Arrighetti, Paola Perego*Diego Colombo
Affiliation:
- Molecular Pharmacology Unit, Department of Applied Research and Technological Development,
Fondazione IRCCS Istituto Nazionale dei Tumori, Milan, Italy
Keywords:
Platinum compounds, conjugates, hybrid anticancer agents, tumor targeting, drug resistance, cisplatin.
Abstract: Platinum (Pt) drugs, including cisplatin, are widely used for the treatment of solid
tumors. Despite the clinical success, side effects and occurrence of resistance represent major
limitations to the use of clinically available Pt drugs. To overcome these problems, a variety
of derivatives have been designed and synthetized. Here, we summarize the recent progress
in the development of Pt(II) and Pt(IV) complexes with bioactive ligands. The development
of Pt(II) and Pt(IV) complexes with targeting molecules, clinically available agents, and other
bioactive molecules is an active field of research. Even if none of the reported Pt derivatives
has been yet approved for clinical use, many of these compounds exhibit promising
anticancer activities with an improved pharmacological profile. Thus, planning hybrid compounds
can be considered as a promising approach to improve the available Pt-based anticancer
agents and to obtain new molecular tools to deepen the knowledge of cancer progression
and drug resistance mechanisms.