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Abstract

Introduction

Chemotherapy remains essential despite advances in immunotherapy, radiotherapy, and biological therapy. However, the wide range of chemical drugs is limited by a narrow therapeutic index, low selectivity, and the development of resistance. In this regard, new high-efficiency drugs are in extremely high demand. The indazole moiety, a scaffold found in many biologically active compounds, was selected for use in new drug design.

Methods

Six new indazole derivatives were synthesized Suzuki-Miyaura coupling starting from bromoindazole. Their antiviral (against influenza A and SARS-CoV-2), antibacterial (against ), and antiproliferative activities (against neuroblastoma, glioma, leukemia cell lines) were evaluated . Acute toxicity was assessed in mice of both sexes single intragastric administration, with toxicometric parameters and pathomorphological changes studied.

Results

6-(1H-pyrazol-4-yl)-1H-indazole () suppressed the reproduction of the influenza virus at non-toxic doses to the MDCK cells and showed cytotoxicity against cancer cell lines, with an IC between 4 and 14 µM. However, it exhibited significant acute toxicity in mice (LD 40 mg/kg), causing systemic organ damage.

Discussion

Derivative demonstrated promising antiviral and antiproliferative activities but exhibited considerable acute toxicity . The antiviral efficacy, although lower than oseltamivir, is meaningful and justifies further optimization and investigation. Its antibacterial activity against adds to its potential as a multifunctional agent.

Conclusion

While derivative has shown potential as an antiviral and anticancer agent, its high toxicity highlights the need for further studies to define a safe and effective therapeutic window. Overall, the indazole scaffold remains a valuable platform for the development of new therapeutic compounds.

© 2025 The Author(s). Published by Bentham Science Publishers.
This is an open access article published under CC BY 4.0 https://creativecommons.org/licenses/by/4.0/legalcode
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2025-09-05
2025-11-04

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New Indazole Derivatives as Potential Scaffolds for the Development of Anticancer, Antiviral, and Anti-tuberculosis Chemotherapeutic Compounds
Bentham Science Publishers ; https://doi.org/10.2174/0109298673389070250822065247
/content/journals/cmc/10.2174/0109298673389070250822065247
/content/journals/cmc/10.2174/0109298673389070250822065247
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  • Article Type:     Research Article
Keywords: Mycobacterium tuberculosis ; drug design ; anticancer activity ; antiviral compounds ; Indazole derivatives ; inhibition

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