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Review

Recent Advances in the Application of Nitro(het)aromatic Compounds for Treating and/or Fluorescent Imaging of Tumor Hypoxia

by
Kameliya Anichina
1,
Nikolay Lumov
1,2,
Ventsislav Bakov
1,
Denitsa Yancheva
1,2 and
Nikolai Georgiev
1,*
1
Department of Organic Synthesis, University of Chemical Technology and Metallurgy, 8 Kliment Ohridski Blvd., 1756 Sofia, Bulgaria
2
Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Acad. G. Bonchev str. Bl. 9, 1113 Sofia, Bulgaria
*
Author to whom correspondence should be addressed.
Molecules 2024, 29(15), 3475; https://doi.org/10.3390/molecules29153475
Submission received: 5 June 2024 / Revised: 22 July 2024 / Accepted: 22 July 2024 / Published: 25 July 2024
(This article belongs to the Special Issue Small-Molecule Modulators Targeting Emerging Therapeutic Pathways: Design, Synthesis and Biological Evaluation)
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Abstract

This review delves into recent advancements in the field of nitro(het)aromatic bioreductive agents tailored for hypoxic environments. These compounds are designed to exploit the low-oxygen conditions typically found in solid tumors, making them promising candidates for targeted cancer therapies. Initially, this review focused on their role as gene-directed enzyme prodrugs, which are inert until activated by specific enzymes within tumor cells. Upon activation, these prodrugs undergo chemical transformations that convert them into potent cytotoxic agents, selectively targeting cancerous tissue while sparing healthy cells. Additionally, this review discusses recent developments in prodrug conjugates containing nitro(het)aromatic moieties, designed to activate under low-oxygen conditions within tumors. This approach enhances their efficacy and specificity in cancer treatment. Furthermore, this review covers innovative research on using nitro(het)aromatic compounds as fluorescent probes for imaging hypoxic tumors. These probes enable non-invasive visualization of low-oxygen regions within tumors, providing valuable insights for the diagnosis, treatment planning, and monitoring of therapeutic responses. We hope this review will inspire researchers to design and synthesize improved compounds for selective cancer treatment and early diagnostics.
Keywords: nitroaromatic compounds; hypoxia; tumor treatment; fluorescence imaging nitroaromatic compounds; hypoxia; tumor treatment; fluorescence imaging
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MDPI and ACS Style

Anichina, K.; Lumov, N.; Bakov, V.; Yancheva, D.; Georgiev, N. Recent Advances in the Application of Nitro(het)aromatic Compounds for Treating and/or Fluorescent Imaging of Tumor Hypoxia. Molecules 2024, 29, 3475. https://doi.org/10.3390/molecules29153475

AMA Style

Anichina K, Lumov N, Bakov V, Yancheva D, Georgiev N. Recent Advances in the Application of Nitro(het)aromatic Compounds for Treating and/or Fluorescent Imaging of Tumor Hypoxia. Molecules. 2024; 29(15):3475. https://doi.org/10.3390/molecules29153475

Chicago/Turabian Style

Anichina, Kameliya, Nikolay Lumov, Ventsislav Bakov, Denitsa Yancheva, and Nikolai Georgiev. 2024. "Recent Advances in the Application of Nitro(het)aromatic Compounds for Treating and/or Fluorescent Imaging of Tumor Hypoxia" Molecules 29, no. 15: 3475. https://doi.org/10.3390/molecules29153475

APA Style

Anichina, K., Lumov, N., Bakov, V., Yancheva, D., & Georgiev, N. (2024). Recent Advances in the Application of Nitro(het)aromatic Compounds for Treating and/or Fluorescent Imaging of Tumor Hypoxia. Molecules, 29(15), 3475. https://doi.org/10.3390/molecules29153475

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