Related Experiment Video
Updated: Jan 17, 2026
Studying Triple Negative Breast Cancer Using Orthotopic Breast Cancer Model
Published on: March 20, 2020
Synthesis and Evaluation of Novel Fluorinated Quinoline Derivatives in 2D and 3D Models of Triple-Negative Breast
Anubha Yadav1, Sachin Saini2, Mamta Singh1
1Amity Institute of Molecular Medicine and Stem Cell Research, Amity University Noida, Uttar Pradesh 201303, India.
Abstract:
Triple-negative breast cancer (TNBC) is a particularly aggressive subtype of breast cancer that is more likely to metastasize and become resistant with a worse prognosis. Herein, we have synthesized novel fluorinated quinoline analogues and investigated their anticancer properties against breast cancer cell lines and cancer cell spheroids. Compounds 6a, 6b, 6d, and 6f demonstrated potent anticancer activity with IC50 values of 2.5-5 μM against TNBC cells (MDA-MB-468), while remaining nontoxic to nontumorigenic breast cells (MCF-10A). The hydrolyzed analogues 7a-f were not active against TNBC cells, implying that the ester group together with fluorine substitution on the quinoline ring is critical for their anticancer activity. Compounds 6a, 6b, and 6f significantly reduced the clonogenic capacity of TNBC cells and induced reactive oxygen species (ROS). Notably, compounds 6b and 6f considerably decreased TNBC cells (MDA-MB-468 and 4T1) 3D spheroids volume. The present research opens new avenues for developing novel therapeutics for breast cancers.
Insights
Novel fluorinated quinoline compounds show potent anticancer activity against triple-negative breast cancer (TNBC) cells. These compounds effectively reduced tumor cell growth and spheroid volume without harming normal breast cells, offering new therapeutic potential.
Area of Science:
- Medicinal Chemistry
- Oncology
- Drug Discovery
Background:
- Triple-negative breast cancer (TNBC) is an aggressive subtype with poor prognosis and high resistance.
- Developing novel therapeutics for TNBC remains a critical unmet need.
Purpose of the Study:
- To synthesize novel fluorinated quinoline analogues.
- To evaluate their anticancer properties against breast cancer cell lines and spheroids.
- To identify key structural features for anticancer activity.
Main Methods:
- Synthesis of fluorinated quinoline analogues.
- In vitro evaluation of cytotoxicity against TNBC and normal breast cells.
- Assessment of clonogenic capacity and reactive oxygen species (ROS) induction.
- 3D spheroid culture models to evaluate efficacy.
Main Results:
- Compounds 6a, 6b, 6d, and 6f exhibited potent activity against TNBC cells (IC50: 2.5-5 μM) with no toxicity to normal cells.
- Hydrolyzed analogues (7a-f) lacked activity, highlighting the importance of the ester and fluorine groups.
- Active compounds reduced clonogenic capacity, induced ROS, and significantly decreased 3D spheroid volume in TNBC models.
- Compounds 6b and 6f were particularly effective against MDA-MB-468 and 4T1 TNBC cell lines.
Conclusions:
- Fluorinated quinoline analogues demonstrate significant potential as anticancer agents for TNBC.
- The ester group and fluorine substitution are crucial for the observed anticancer effects.
- These findings pave the way for developing new TNBC therapeutics.
