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Updated: Mar 29, 2026
Studying Triple Negative Breast Cancer Using Orthotopic Breast Cancer Model
Published on: March 20, 2020
Ultrasound-Assisted Synthesis and Biological Profiling of 1,3,5-Triazine Derivatives with Antiproliferative Activity
Natalia Bosak1, Anna Karolina Drabczyk1, Jolanta Jaśkowska1
1Department of Organic Chemistry and Technology, Faculty of Chemical Engineering and Technology, Cracow University of Technology, 24 Warszawska Street, 31-155 Cracow, Poland.
Abstract:
Triple-negative breast cancer (TNBC) remains one of the most aggressive breast cancer subtypes and is associated with limited therapeutic options, underscoring the urgent need for novel treatment strategies. In this study, a library of seventeen 1,3,5-triazine derivatives potentially targeting TNBC was developed using an activity-based approach. Compounds were synthesized via an ultrasound-assisted protocol, providing an efficient and environmentally friendly methodology. The synthesized library was evaluated in vitro against the human TNBC cell lines MDA-MB-468, MDA-MB-231, and Hs578T, as well as the non-tumorigenic epithelial cell line MCF10A. Compounds 9 and 17 exhibited the most promising antiproliferative activity against TNBC cell lines (MDA-MB-468: IC50 = 36.62 µM for 9 and 38.29 µM for 17; MDA-MB-231: IC50 = 37.32 µM for 9 and 32.86 µM for 17; Hs578T: IC50 = 57.26 µM for 9 and 34.87 µM for 17), while maintaining acceptable selectivity toward non-cancerous cells. The lead compounds were further assessed in vivo using a Danio rerio model to evaluate general toxicity and cardiotoxicity. In addition, ADME parameters were predicted for all compounds using biomimetic chromatography. Overall, compounds 9 and 17 emerged as promising small-molecule candidates for TNBC treatment, requiring further toxicological evaluation in more human-relevant in vivo models.
Insights
Researchers developed novel 1,3,5-triazine derivatives to treat triple-negative breast cancer (TNBC). Compounds 9 and 17 show promising antiproliferative activity against TNBC cells and require further study for potential therapeutic use.
Area of Science:
- Medicinal Chemistry
- Oncology
- Drug Discovery
Background:
- Triple-negative breast cancer (TNBC) is an aggressive subtype with limited treatment options.
- There is an urgent need for novel therapeutic strategies to combat TNBC.
- 1,3,5-triazine derivatives represent a potential class of compounds for TNBC treatment.
Purpose of the Study:
- To synthesize and evaluate a library of 1,3,5-triazine derivatives for antiproliferative activity against TNBC.
- To identify lead compounds with potent activity and acceptable selectivity.
- To perform preliminary in vivo and in silico assessments of lead compounds.
Main Methods:
- Synthesis of seventeen 1,3,5-triazine derivatives using an ultrasound-assisted protocol.
- In vitro antiproliferative activity assessment against TNBC cell lines (MDA-MB-468, MDA-MB-231, Hs578T) and a non-tumorigenic cell line (MCF10A).
- In vivo toxicity assessment in a Danio rerio model and ADME parameter prediction using biomimetic chromatography.
Main Results:
- Compounds 9 and 17 demonstrated significant antiproliferative activity against all tested TNBC cell lines.
- IC50 values for compounds 9 and 17 ranged from 32.86 µM to 57.26 µM against TNBC cells.
- Lead compounds exhibited acceptable selectivity towards non-cancerous cells and showed no significant general or cardiotoxicity in the Danio rerio model.
Conclusions:
- Compounds 9 and 17 are promising small-molecule candidates for TNBC treatment.
- Further toxicological evaluation in more human-relevant in vivo models is warranted.
- The developed ultrasound-assisted synthesis protocol is efficient and environmentally friendly.
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