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Article

Synthesis and Evaluation of Boron-Containing Heterocyclic Compounds with Antimicrobial and Anticancer Activities

by
João Lucas Bruno Prates
1,2,*,
Samanta de Matos Silva
1,
Kaila Petrolina Medina-Alarcón
1,
Kelvin Sousa dos Santos
1,
Jenyffie Araujo Belizario
1,
Juliana Romano Lopes
1,
Freddy Humberto Marin-Dett
1,
Debora Leite Campos
1,
Maria José Soares Mendes Giannini
1,
Ana Marisa Fusco-Almeida
1,
Paula Aboud Barbugli
1,3,
Fernando Rogério Pavan
1 and
Jean Leandro Dos Santos
1,2,*
1
School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara 14800-903, SP, Brazil
2
Institute of Chemistry, São Paulo State University (UNESP), Araraquara 14800-900, SP, Brazil
3
School of Dentistry, São Paulo State University (UNESP), Araraquara 14801-385, SP, Brazil
*
Authors to whom correspondence should be addressed.
Molecules 2025, 30(5), 1117; https://doi.org/10.3390/molecules30051117
Submission received: 13 January 2025 / Revised: 19 February 2025 / Accepted: 24 February 2025 / Published: 28 February 2025
(This article belongs to the Special Issue Advances in the Synthesis of Heterocyclic Compounds and Their Applications)
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Abstract

Organoboron compounds, especially those containing boronic acid and benzoxaborole in their structure, have been gaining prominence in medicinal chemistry, following the FDA approval of tavaborole for the treatment of onychomycosis and bortezomib for multiple myeloma. The antimicrobial and anticancer effects of organoboron compounds motivate the investigation of the effects of the novel derivatives described here. A total of fourteen new boronic derivatives were synthesized and characterized using analytical methods. The antimicrobial activities were evaluated against M. tuberculosis (Mtb) H37Rv strains and fungal dermatophytes (C. albicans, ATCC 90028; T. rubrum, ATCC 28189; and T. mentagrophytes, ATCC 11481), while the anticancer effect was evaluated against oral squamous cell carcinoma (SCC) cell lines. Several promising boron-containing prototypes were identified, providing a foundation for further molecular optimization in the development of new antimicrobial and anticancer compounds.
Keywords: organoboron; boronic acid; benzoxaborole; boron-containing compounds; Mycobacterium tuberculosis; antimicrobial; fungi; cancer organoboron; boronic acid; benzoxaborole; boron-containing compounds; Mycobacterium tuberculosis; antimicrobial; fungi; cancer
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MDPI and ACS Style

Prates, J.L.B.; de Matos Silva, S.; Medina-Alarcón, K.P.; dos Santos, K.S.; Belizario, J.A.; Lopes, J.R.; Marin-Dett, F.H.; Campos, D.L.; Mendes Giannini, M.J.S.; Fusco-Almeida, A.M.; et al. Synthesis and Evaluation of Boron-Containing Heterocyclic Compounds with Antimicrobial and Anticancer Activities. Molecules 2025, 30, 1117. https://doi.org/10.3390/molecules30051117

AMA Style

Prates JLB, de Matos Silva S, Medina-Alarcón KP, dos Santos KS, Belizario JA, Lopes JR, Marin-Dett FH, Campos DL, Mendes Giannini MJS, Fusco-Almeida AM, et al. Synthesis and Evaluation of Boron-Containing Heterocyclic Compounds with Antimicrobial and Anticancer Activities. Molecules. 2025; 30(5):1117. https://doi.org/10.3390/molecules30051117

Chicago/Turabian Style

Prates, João Lucas Bruno, Samanta de Matos Silva, Kaila Petrolina Medina-Alarcón, Kelvin Sousa dos Santos, Jenyffie Araujo Belizario, Juliana Romano Lopes, Freddy Humberto Marin-Dett, Debora Leite Campos, Maria José Soares Mendes Giannini, Ana Marisa Fusco-Almeida, and et al. 2025. "Synthesis and Evaluation of Boron-Containing Heterocyclic Compounds with Antimicrobial and Anticancer Activities" Molecules 30, no. 5: 1117. https://doi.org/10.3390/molecules30051117

APA Style

Prates, J. L. B., de Matos Silva, S., Medina-Alarcón, K. P., dos Santos, K. S., Belizario, J. A., Lopes, J. R., Marin-Dett, F. H., Campos, D. L., Mendes Giannini, M. J. S., Fusco-Almeida, A. M., Barbugli, P. A., Pavan, F. R., & Dos Santos, J. L. (2025). Synthesis and Evaluation of Boron-Containing Heterocyclic Compounds with Antimicrobial and Anticancer Activities. Molecules, 30(5), 1117. https://doi.org/10.3390/molecules30051117

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