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A tutorial for the assessment of the stability of organometallic complexes in biological media
Journal of Organometallic Chemistry ( IF 2.3 ) Pub Date : 2019-12-02 , DOI: 10.1016/j.jorganchem.2019.121059
Sarah Keller , Yih Ching Ong , Yan Lin , Kevin Cariou , Gilles Gasser

The use of metal-based drugs is increasingly gaining importance in medicine and renowned conferences such as the International Symposium on Bioorganometallic Chemistry (ISBOMC) are excellent opportunities for scientists in the field to exchange ideas and present their research on this topic. We decided to dedicate one of our group's presentations at ISBOMC′19 to the detailed experimental description of the stability studies on metallocene-containing compounds that we are currently developing. The stability of (organometallic) drug candidates in biological media such as plasma is indeed a crucial parameter in medicinal chemistry and drug design. The presentation was very well received by the audience, which prompted us to contribute to this special issue with an article in the form of a tutorial. More specifically, we are aiming to show how such experiments can be easily performed in standard chemistry laboratories, without the need of specific pharmacological or biological expertise. In this tutorial article, we describe the detailed protocols for studies with human plasma and human microsomes, which simulate the conditions in the blood and liver, respectively, so that medicinal chemists from organometallic backgrounds can take the plunge without fear.



中文翻译:

用于评估生物介质中有机金属配合物稳定性的教程

金属基药物的使用在医学中变得越来越重要,诸如国际生物金属有机化学研讨会(ISBOMC)之类的著名会议为该领域的科学家提供了交流思想并介绍他们在该主题上的研究的绝好机会。我们决定将小组在ISBOMC'19上的演讲之一专门用于对我们目前正在开发的含茂金属化合物的稳定性研究进行详细的实验描述。(有机金属)候选药物在生物介质(例如血浆)中的稳定性确实是药物化学和药物设计中的关键参数。该演示文稿受到了观众的好评,这促使我们以教程形式的文章为这一特殊问题做出了贡献。进一步来说,我们旨在展示如何在标准化学实验室中轻松进行此类实验,而无需特定的药理或生物学专业知识。在本教程文章中,我们描述了使用人体血浆和人体微粒体进行研究的详细协议,它们分别模拟了血液和肝脏中的状况,因此来自有机金属背景的药物化学家可以毫不犹豫地进行尝试。

更新日期:2019-12-02
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