Synthesis and Evaluation of Boron-Containing Heterocyclic Compounds with Antimicrobial and Anticancer Activities
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 <i>M. tuberculosis</i> (<i>Mtb</i>) H37Rv strains and fungal dermatophytes (<i>C. albicans</i>, ATCC 90028; <i>T. rubrum</i>, ATCC 28189; and <i>T. mentagrophytes</i>, 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.
Authors
- Ana Marisa Fusco‐Almeida (ORCID: https://orcid.org/0000-0002-2115-8988)
- Kelvin Sousa dos Santos (ORCID: https://orcid.org/0000-0001-8328-9054)
- Jean Leandro dos Santos (ORCID: https://orcid.org/0000-0002-2460-2829)
- João Lucas Bruno Prates (ORCID: https://orcid.org/0000-0003-0187-4626)
- Fernando Rogerio Pavan (ORCID: https://orcid.org/0000-0002-6969-3963)
- Samanta de Matos Silva (ORCID: https://orcid.org/0000-0002-1390-117X)
- Paula Aboud Barbugli (ORCID: https://orcid.org/0000-0002-0078-1172)
- Freddy Humberto Marin-Dett (ORCID: https://orcid.org/0000-0002-6979-625X)
- Maria José Soares Mendes‐Giannini (ORCID: https://orcid.org/0000-0002-8059-0826)
- Jenyffie Araújo Belizário
- Débora L. Campos (ORCID: https://orcid.org/0000-0003-2250-8342)
- Juliana Romano Lopes (ORCID: https://orcid.org/0000-0002-3141-501X)
- Kaila Petrolina Medina-Alarcón
Institutions
- Universidade Estadual Paulista (Unesp) (BR)
Publication Details
- Journal
- Molecules
- Published
- 2025-02-28
- DOI
- https://doi.org/10.3390/molecules30051117
- Citations
- 5
- Primary Topic
- Organoboron and organosilicon chemistry
- Type
- article
- Field-Weighted Citation Impact
- 4.68
Funders
- Fundação de Amparo à Pesquisa do Estado de São Paulo
- Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
- Conselho Nacional de Desenvolvimento Científico e Tecnológico