Chemistry, structure, and biological roles of Au-NHC complexes as TrxR inhibitors.,Bioorganic Chemistry

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Chemistry, structure, and biological roles of Au-NHC complexes as TrxR inhibitors.
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2019-12-24 , DOI: 10.1016/j.bioorg.2019.103552
Merve Gökşin Karaaslan ₁ , Aydın Aktaş ₁ , Canbolat Gürses ₂ , Yetkin Gök ₁ , Burhan Ateş ₁

Affiliation

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.

中文翻译：

Au-NHC复合物作为TrxR抑制剂的化学，结构和生物学作用。

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，通常将N-杂环药剂用作有希望的核。含金的N-杂环卡宾（Au-NHC）衍生物是用于此目的的化合物，并且对其酶抑制，抗氧化活性，抗微生物和抗癌性能进行了广泛的研究。在这些研究中，Au-NHC复合物的抗癌特性是研究最广泛的领域。在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复合物强大的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影响的主要成分。这篇综述包括与Au-NHC化合物的抗癌活性和TrxR抑制特性有关的讨论。

更新日期：2019-12-25

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