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Updated: Jan 29, 2026
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Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
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Benzotriazole in Cancer: A Systematic Review on Preclinical Evidence and Structure-Activity Relationship
Gabriel Mardale1,2, Alexandra Prodea1,2, Andreea Munteanu1,2
1Faculty of Pharmacy, "Victor Babes" University of Medicine and Pharmacy, Eftimie Murgu Square, No. 2, 300041 Timișoara, Romania.
Pharmaceuticals (Basel, Switzerland)
|January 28, 2026
Summary
Benzotriazole derivatives show promise as anticancer agents, exhibiting cytotoxicity and reducing tumor mass in preclinical studies. Further research with rigorous methods is needed to confirm their therapeutic potential and safety.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Drug Discovery
Background:
- Benzotriazoles are versatile heterocycles in medicinal chemistry.
- Benzotriazole derivatives are explored as potent anticancer drug candidates.
- A comprehensive review of preclinical benzotriazole anticancer studies is lacking.
Purpose of the Study:
- To review preclinical evidence on benzotriazole derivatives as anticancer agents.
- To focus on cytotoxicity, mechanisms of action, structure-activity relationships, and methodological rigor.
- To identify promising benzotriazole derivatives for cancer treatment.
Main Methods:
- Systematic literature search of PubMed, Scopus, and Web of Science.
- Inclusion of 41 studies based on selection criteria.
- Risk of bias assessment using QUIN (in vitro) and SYRCLE (in vivo) tools.
Main Results:
- Benzotriazole derivatives classified into N-, C-, fused, and organometallic compounds.
- In vitro studies showed superior cytotoxicity via apoptosis and cell cycle arrest.
- In vivo studies demonstrated dose-dependent tumor mass reduction with minimal hepatotoxicity.
Conclusions:
- Benzotriazole derivatives are promising anticancer candidates.
- Limited mechanistic and toxicity data, along with moderate risk of bias, necessitate caution.
- Future studies require rigorous methodologies to fully assess therapeutic potential and safety.
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