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Towards anticancer fluoroquinolones: A review article

Mohamed A A Abdel-Aal1,2, Salah A Abdel-Aziz2, Montaser Sh A Shaykoon2

  • 1Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, Minia, Egypt.

Archiv Der Pharmazie
|June 20, 2019
PubMed

Insights

Antibacterial fluoroquinolones show anticancer potential by targeting human DNA topoisomerases. Chemical modifications at specific positions and metal ion chelation enhance their antitumor activity, aiding the development of novel cancer drugs.

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Oncology

Background:

  • Antibacterial fluoroquinolones possess anticancer properties.
  • Their mechanism involves poisoning type II human DNA topoisomerases, similar to some chemotherapy agents.
  • Structural modifications are key to converting antibacterial fluoroquinolones into anticancer drugs.

Purpose of the Study:

  • To review the antitumor potential of fluoroquinolones.
  • To summarize chemical modifications enhancing anticancer activity.
  • To highlight the role of metal ion chelates in improving topoisomerase poisoning and antitumor effects.

Main Methods:

  • Literature review of studies on fluoroquinolone anticancer activity.
  • Analysis of structural modifications at positions 3 and 7.
  • Examination of metal ion chelation strategies.

Main Results:

  • Fluoroquinolones can be modified to exhibit significant antitumor activity.
  • Specific structural changes, particularly at position 7 and the carboxylic group at position 3, are crucial.
  • Metal ion chelation enhances topoisomerase poisoning and overall anticancer efficacy.

Conclusions:

  • Fluoroquinolones represent a promising scaffold for novel anticancer drug development.
  • Targeted chemical modifications and metal complexation are effective strategies to optimize their therapeutic potential.
  • This review provides insights for designing next-generation fluoroquinolone-based anticancer agents.
Keywords:
DNA topoisomeraseanticancermetal ion complexesquinolones

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