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Abstract

Synthetically Enhanced Betulin-Based Triazoles as Promising Anticancer Agents †

by
Alexandra Prodea
1,2,
Oana Eşanu
1,2,*,
Marius Mioc
1,2 and
Codruța Șoica
1,2
1
Faculty of Pharmacy, Victor Babes University of Medicine and Pharmacy, 300041 Timișoara, Romania
2
Research Center for Experimental Pharmacology and Drug Design, Victor Babes University of Medicine and Pharmacy, 300041 Timișoara, Romania
*
Author to whom correspondence should be addressed.
†
Presented at the International Conference on Interdisciplinary Approaches and Emerging Trends in Pharmaceutical Doctoral Research: Innovation and Integration, Timisoara, Romania, 7–9 July 2025.
Proceedings 2025, 127(1), 12; https://doi.org/10.3390/proceedings2025127012
Published: 24 September 2025
(This article belongs to the Proceedings of International Conference on Interdisciplinary Approaches and Emerging Trends in Pharmaceutical Doctoral Research: Innovation and Integration)
Versions Notes

This study presents the synthesis and biological evaluation of novel betulin-based 1,2,4-triazole derivatives targeting human cancer cells. The compounds were obtained following the alkylation of 30-bromo-3,28-O-acetyl-betulin with various 5-R-1,2,4-triazole-3-thiols [1]. Through these chemical modifications at the C30 position, four derivatives (Bet-TZ1-4) were obtained. The structure of the obtained compounds was validated through 1D and 2D NMR, FTIR, and LC-MS, and subsequently assessed for their in vitro antiproliferative activity against the A375 (melanoma), MCF-7 (breast cancer), and HT-29 (colorectal cancer) cell lines, alongside non-tumorigenic HaCaT keratinocytes. Bet-TZ1 and Bet-TZ3 demonstrated dose-dependent cytotoxic effects, with Bet-TZ1 showing the lowest IC50 values across all cancer cell lines, notably superior to its precursor and the reference compound 5-fluorouracil. Morphological and nuclear staining assays confirmed apoptosis induction, supported by elevated caspase 9 expression. Migration assays further highlighted the inhibitory effect of Bet-TZ1 on cell motility. Importantly, no significant irritative potential was observed in the HET-CAM assay. These findings support the continued exploration of triazole-modified phytocompounds as selective anticancer agents with enhanced efficacy and safety profiles.

Author Contributions

Conceptualization, A.P., M.M. and C.Ș.; methodology, A.P., O.E., M.M. and C.Ș.; software, A.P. and M.M.; validation, A.P. and M.M.; formal analysis, A.P., M.M.; investigation, A.P., O.E. and M.M.; resources, A.P.; data curation A.P. and O.E.; writing-original draft preparation, A.P., O.E., M.M. and C.Ș.; writing-review and editing, A.P., O.E., M.M. and C.Ș., visualization, A.P. and O.E.; supervision, M.M. and C.Ș.; project administration, A.P., M.M. and C.Ș.; funding acquisition, A.P., M.M. All authors have read and agreed to the published version of the manuscript.

Funding

This research was funded by the University of Medicine and Pharmacy “Victor Babes” Timisoara, grant number 26679/09.11.2022 (M.M.).

Institutional Review Board Statement

Not applicable.

Informed Consent Statement

Not applicable.

Data Availability Statement

The original contributions presented in the study are included in the manuscript, further inquiries can be directed to the corresponding author.

Conflicts of Interest

The authors declare no conflict of interest.

Reference

  1. Prodea, A.; Milan, A.; Mioc, M.; Mioc, A.; Oprean, C.; Racoviceanu, R.; Negrea-Ghiulai, R.; Mardale, G.; Avram, Ș.; Balan-Porcărașu, M.; et al. Novel Betulin-1,2,4-Triazole Derivatives Promote In Vitro Dose-Dependent Anticancer Cytotoxicity. Processes 2024, 12, 24. [Google Scholar] [CrossRef]
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MDPI and ACS Style

Prodea, A.; Eşanu, O.; Mioc, M.; Șoica, C. Synthetically Enhanced Betulin-Based Triazoles as Promising Anticancer Agents. Proceedings 2025, 127, 12. https://doi.org/10.3390/proceedings2025127012

AMA Style

Prodea A, Eşanu O, Mioc M, Șoica C. Synthetically Enhanced Betulin-Based Triazoles as Promising Anticancer Agents. Proceedings. 2025; 127(1):12. https://doi.org/10.3390/proceedings2025127012

Chicago/Turabian Style

Prodea, Alexandra, Oana Eşanu, Marius Mioc, and Codruța Șoica. 2025. "Synthetically Enhanced Betulin-Based Triazoles as Promising Anticancer Agents" Proceedings 127, no. 1: 12. https://doi.org/10.3390/proceedings2025127012

APA Style

Prodea, A., Eşanu, O., Mioc, M., & Șoica, C. (2025). Synthetically Enhanced Betulin-Based Triazoles as Promising Anticancer Agents. Proceedings, 127(1), 12. https://doi.org/10.3390/proceedings2025127012

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