具有抗菌和抗癌活性的含硼杂环化合物的合成与评价
Synthesis and Evaluation of Boron-Containing Heterocyclic Compounds with Antimicrobial and Anticancer Activities.
作者信息
Prates João Lucas Bruno, de Matos Silva Samanta, Medina-Alarcón Kaila Petrolina, Dos Santos Kelvin Sousa, Belizario Jenyffie Araujo, Lopes Juliana Romano, Marin-Dett Freddy Humberto, Campos Debora Leite, Mendes Giannini Maria José Soares, Fusco-Almeida Ana Marisa, Barbugli Paula Aboud, Pavan Fernando Rogério, Dos Santos Jean Leandro
机构信息
School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara 14800-903, SP, Brazil.
Institute of Chemistry, São Paulo State University (UNESP), Araraquara 14800-900, SP, Brazil.
出版信息
Molecules. 2025 Feb 28;30(5):1117. doi: 10.3390/molecules30051117.
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 () H37Rv strains and fungal dermatophytes (, ATCC 90028; , ATCC 28189; and , 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.
在他伏硼罗获美国食品药品监督管理局（FDA）批准用于治疗甲癣以及硼替佐米获批准用于治疗多发性骨髓瘤之后，有机硼化合物，尤其是那些结构中含有硼酸和苯并氧杂硼杂环戊二烯的有机硼化合物，在药物化学领域日益受到关注。有机硼化合物的抗菌和抗癌作用促使人们对本文所述新型衍生物的作用进行研究。总共合成了14种新的硼酸衍生物，并采用分析方法对其进行了表征。针对结核分枝杆菌H37Rv菌株和皮肤癣菌（红色毛癣菌，ATCC 90028；须癣毛癣菌，ATCC 28189；疣状毛癣菌，ATCC 11481）评估了抗菌活性，同时针对口腔鳞状细胞癌（SCC）细胞系评估了抗癌效果。确定了几种有前景的含硼原型，为开发新型抗菌和抗癌化合物的进一步分子优化奠定了基础。
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