Laboratory of Biomedical Chemistry, Hirszfeld Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, 53-114 Wrocław, Poland.
J Med Chem. 2024 Jun 13;67(11):8481-8501. doi: 10.1021/acs.jmedchem.4c00157. Epub 2024 May 21.
Metallacarboranes, exemplified by cobalt bis(dicarbollide) ([COSAN]), have excelled their historical metallocene analogue label to become promising in drug design, medical studies, and fundamental biological research. Serving as a unique platform for conjugation with biomolecules, they also constitute an auspicious building block for biologically active derivatives and a carrier for cellular transport of membrane-impermeable cargos. Modified [COSAN] exhibits specific antimicrobial, antiviral, and anticancer actions showing promise for preclinical trials. Contributing to the ongoing development in medicinal chemistry, metallacarboranes offer desirable physicochemical properties and low acute toxicity. This article presents a critical look at metallacarboranes in the context of their application in medicinal chemistry, emphasizing [COSAN] as a potential game-changer in drug design and biomedical sciences. As medicinal chemistry seeks innovative building blocks, metallacarboranes emerge as an important novelty with versatile solutions and promising implications.
金属碳硼烷，以双(碳硼烷)合钴([COSAN])为例，超越了其历史上的金属茂类似物标签，在药物设计、医学研究和基础生物学研究中具有广阔的应用前景。作为与生物分子结合的独特平台，它们也是生物活性衍生物的良好构建块，也是膜不可渗透货物细胞运输的载体。修饰的[COSAN]表现出特定的抗微生物、抗病毒和抗癌作用，有望进行临床前试验。为药物化学的不断发展做出贡献，金属碳硼烷具有理想的物理化学性质和低急性毒性。本文从药物化学应用的角度对金属碳硼烷进行了批判性的研究，强调[COSAN]作为药物设计和生物医学科学的潜在变革者的潜力。随着药物化学寻求创新的构建模块，金属碳硼烷作为一种具有多功能解决方案和广阔前景的重要新颖性出现。
