Abstract

Platinum-based anticancer drugs represented by cisplatin play important roles in the treatment of various solid tumors. However, their applications are largely compromised by drug resistance and side effects. Much effort has been made to circumvent the drug resistance and general toxicity of these drugs. Among multifarious designs, monofunctional platinum(II) complexes with a general formula of [Pt(3A)Cl]+ (A: Ammonia or amine) stand out as a class of “non-traditional” anticancer agents hopeful to overcome the defects of current platinum drugs. This review aims to summarize the development of monofunctional platinum(II) complexes in recent years. They are classified into four categories: fluorescent complexes, photoactive complexes, targeted complexes, and miscellaneous complexes. The intention behind the designs is either to visualize the cellular distribution, or to reduce the side effects, or to improve the tumor selectivity, or inhibit the cancer cells through non-DNA targets. The information provided by this review may inspire researchers to conceive more innovative complexes with potent efficacy to shake off the drawbacks of platinum anticancer drugs.

Highlights

  • IntroductionCisplatin and and its its analogues, analogues, carboplatin, carboplatin, oxaliplatin, oxaliplatin, nedaplatin [1], lobaplatin [2], Cisplatin and1) have havebeen beenapproved approvedfor forclinical clinicaluse useinindifferent different countries and heptaplatin heptaplatin [3] (Figure 1)countries to to treat multiplesolid solidneoplasms, neoplasms,and andapproximately approximatelyhalf half of of the chemotherapy treat multiple chemotherapy strategies strategies include include platinum platinum drugs drugs [4,5,6].[4,5,6]

  • Porphyrins are representative PSs for Photodynamic therapy (PDT) owing to the ring structure with 18 conjugated π electrons, which endow the compounds with photophysical properties and selective retention or accumulation in tumors due to preferential binding to low density lipoproteins [53,54]

  • Pt-based drugs play an important part in cancer therapeutic regimens, play toxic an important part in cancer therapeutic their widespreadAlthough use is still Pt-based limited bydrugs the severe side effects arising from the lack of regimens, their widespread use is still limited by the severe toxic side effects arising from the lack selectivity for cancer cells

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Summary

22 School

Theseauthors authorscontributed contributedequally equallyto tothis thisarticle. article. Platinum(II) Anticancer Agents. Pharmaceuticals 2021, 14, x. Publisher’s Note: MDPI stays neuPublisher’s Note: MDPI stays neutral tral with regard to jurisdictional with regard to jurisdictional claims in claims in published maps and institupublished maps and institutional affiltional affiliations. iations.

Introduction
Chemical
Fluorescent Monofunctional PtII Complexes
Photoactive Monofunctional PtII Complexes
10 Complex 10 efficient 1owing
Targeted Monofunctional PtII Complexes
10. Chemical
11. Chemical
13. Chemical
14. Chemical
Miscellaneous
16. Chemical
Findings
Conclusions

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