The Quinolone Family: From Antibacterial to Anticancer Agents

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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The Quinolone Family: From Antibacterial to Anticancer Agents

Anti-Cancer Agents in Medicinal Chemistry, 3(6): 439-450.

Author(s): Claudia Sissi and Manlio Palumbo.

Affiliation: Dept. of Pharmaceutical Sciences, V. Marzolo 5, 35100 Padova, Italy.


The present review focuses on the structural modifications responsible for the transformation of an antibacterial into an anticancer agent. Indeed, a distinctive feature of drugs based on the quinolone structure is their remarkable ability to target different type II topoisomerase enzymes. In particular, some congeners of this drug family display high activity not only against bacterial topoisomerases, but also against eukaryotic topoisomerases and are toxic to cultured mammalian cells and in vivo tumor models. Hence, these cytotoxic quinolones represent an exploitable source of new anticancer agents, which might also help addressing side-toxicity and resistance phenomena. Their ability to bind metal ion cofactors represents an additional means of modulating their pharmacological response(s). Moreover, quinolones link antibacterial and anticancer chemotherapy together and provide an opportunity to clarify drug mechanism across divergent species.


quinolone family, antibacterial, anticancer agents, type II topoisomerase enzymes, topoisomerases, cytotoxic quinolones, anticancer chemotherapy.

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Article Details

Volume: 3
Issue Number: 6
First Page: 439
Last Page: 450
Page Count: 12
DOI: 10.2174/1568011033482279
Price: $58
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