Related Experiment Video

Updated: Aug 21, 2026

Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?
14:20

Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?

Published on: June 13, 2014

A Rationally Engineered Norfloxacin-Phenoxazine Hybrid as a Dual-Function Anticancer Agent: DNA Intercalation

Rubi Roy1, Tasnim Ria1, Koyel Das1

  • 1Department of Clinical and Translational Research, Chittaranjan National Cancer Institute, 37 S.P. Mukherjee Road, Kolkata 700026 West Bengal, India.

ACS Medicinal Chemistry Letters
|August 20, 2026
PubMed

Insights

New hybrid molecules combining norfloxacin with DNA-targeting agents show potent breast cancer cell killing. These compounds demonstrated significant tumor reduction in vivo with no observed organ toxicity, offering a promising new therapeutic strategy.

Area of Science:

  • Medicinal Chemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Breast cancer treatment faces challenges from drug resistance and systemic toxicity.
  • Novel therapeutic strategies are crucial to overcome these limitations.

Purpose of the Study:

  • To synthesize and evaluate novel hybrid molecules for breast cancer therapy.
  • To investigate the mechanism of action and in vivo efficacy of these hybrids.

Main Methods:

  • Synthesis of norfloxacin-phenoxazine/phenothiazine hybrids.
  • In vitro cytotoxicity assays (MCF-7 cells), DNA intercalation studies, molecular docking.
  • Cell cycle analysis, apoptosis assays, DNA damage assessment (γH2AX).
  • Topoisomerase II inhibition assays and in vivo tumor regression studies.

Main Results:

  • Hybrid compounds demonstrated selective cytotoxicity against breast cancer cells, with compound 4 showing superior potency.
  • Mechanism involves DNA intercalation, topoisomerase II inhibition, cell cycle arrest, and apoptosis induction.
  • In vivo studies showed significant tumor regression for compounds 4 and 10 with no significant hepatic or renal toxicity.

Conclusions:

  • Norfloxacin-based hybrids represent a promising new class of anticancer agents.
  • These hybrids effectively target breast cancer cells and exhibit favorable in vivo efficacy and safety profiles.
Keywords:
AntitumorDNA-intercalatingNorfloxacinPhenoxazineTopoisomerase II

More Related Videos

Potentiation of Anticancer Antibody Efficacy by Antineoplastic Drugs: Detection of Antibody-drug Synergism Using the Combination Index Equation15:04

Potentiation of Anticancer Antibody Efficacy by Antineoplastic Drugs: Detection of Antibody-drug Synergism Using the Combination Index Equation

Published on: January 19, 2019

Sample Extraction and Simultaneous Chromatographic Quantitation of Doxorubicin and Mitomycin C Following Drug Combination Delivery in Nanoparticles to Tumor-bearing Mice08:57

Sample Extraction and Simultaneous Chromatographic Quantitation of Doxorubicin and Mitomycin C Following Drug Combination Delivery in Nanoparticles to Tumor-bearing Mice

Published on: October 5, 2017

Related Concept Videos

Inhibitors of Bacterial DNA Synthesis01:28

Inhibitors of Bacterial DNA Synthesis

Bacterial pathogens depend on precise and efficient DNA replication to sustain infection. Two type II topoisomerases—DNA gyrase and topoisomerase IV—are critical to this process, as they resolve DNA supercoiling and unlink chromosomes during replication. Fluoroquinolones, synthetic derivatives of quinolones, exploit this mechanism by stabilizing the transient DNA–enzyme cleavage complex, preventing strand religation, and causing lethal double-strand breaks. These antibiotics are selectively...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
Treatment Resistant Cancers02:56

Treatment Resistant Cancers

Cancer is the second leading cause of death in the United States. A cancer cell is genetically unstable and hence can mutate faster. They can also modify their microenvironment and escape immune surveillance. The difficulties in treating cancer are further compounded by the emergence of rapid resistance to anticancer drugs. The most common ways to attain resistance in cancer cells include alteration in drug transport and metabolism, modification of drug target, elevated DNA damage response, or...