Benzotriazole in Cancer: A Systematic Review on Preclinical Evidence and Structure–Activity Relationship
Gabriel Mardale, Alexandra Prodea, Andreea Munteanu, Mihaela Jorgovan, Sabina Mardale, Victor Cristian Dumitrascu, Codruța Șoica
TL;DR
This paper reviews preclinical studies on benzotriazole derivatives as potential anticancer agents, highlighting their cytotoxic effects and mechanisms.
Contribution
The study provides a systematic review and structure–activity analysis of benzotriazole compounds in cancer research.
Findings
Benzotriazole derivatives showed superior cytotoxicity through mechanisms like apoptosis and cell cycle arrest.
In vivo studies found tumor mass reduction with minimal hepatotoxicity in some cases.
Limited histopathological data and moderate risk of bias were identified as key limitations.
Abstract
Background: A benzotriazole is a heterocycle frequently used in medicinal chemistry to obtain potent drug candidates, including anticancer agents. Nonetheless, the available literature lacks a comprehensive review of the in vitro and in vivo studies regarding these derivatives. Thus, our study aims to review the preclinical evidence on benzotriazole derivatives that showed potential as anticancer candidates, focusing on the cytotoxicity, mechanisms of action, structure–activity relationship, and methodological rigor of the included studies. Methods: We searched PubMed, Scopus, and Web of Science and included 41 studies in our analysis following the selection process. Additionally, we assessed the risk of bias using the QUIN tool for in vitro and the SYRCLE tool for in vivo studies in order to assess the methodological rigor of the included studies. Results: The benzotriazole derivatives…
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Taxonomy
TopicsSynthesis and biological activity · Cancer therapeutics and mechanisms · Synthesis of Tetrazole Derivatives