Inonu University, Department of Chemistry, 44280 Malatya, Turkey.
Inonu University, Department of Molecular Biology and Genetics, 44280 Malatya, Turkey.
Bioorg Chem. 2020 Jan;95:103552. doi: 10.1016/j.bioorg.2019.103552. Epub 2019 Dec 24.
In recent years, the preparation of metal complexes and the introduction of biologically active organometalic compounds are new strategies in drug development. For this purpose, generally N-heterocyclic pharmaceutical agents have been used as promising nuclei. Au-containing N-heterocyclic carbene (Au-NHC) derivatives are among the compounds used for this purpose, and their enzyme inhibition, antioxidant activity, antimicrobial and anticancer properties are widely studied. In these studies, the anticancer property of Au-NHC complexes is the most widely studied area. The common result in different studies has been revealed that mitochondrial thioredoxin reductases (TrxR) inhibition is the main pathway in the powerful anticancer effect of many Au-NHC complexes. In TrxR inhibition, the high affinity of gold to sulfur is considered to be the main component of the effect. This review includes the discussions releated to the anticancer activities and TrxR inhibition properties of Au-NHC compounds.
近年来,金属配合物的制备和生物活性有机金属化合物的引入是药物开发的新策略。为此,通常使用 N-杂环药物作为有前途的核。含金的 N-杂环卡宾 (Au-NHC) 衍生物就是为此目的而使用的化合物之一,其酶抑制、抗氧化活性、抗菌和抗癌特性得到了广泛研究。在这些研究中,Au-NHC 配合物的抗癌特性是研究最广泛的领域。不同研究中的共同结果表明,线粒体硫氧还蛋白还原酶 (TrxR) 抑制是许多 Au-NHC 配合物强大抗癌作用的主要途径。在 TrxR 抑制中,金对硫的高亲和力被认为是作用的主要组成部分。本文综述了 Au-NHC 化合物的抗癌活性和 TrxR 抑制特性的讨论。