Metallo Nucleosides: Gold Complexes with Antimetabolite Ligands

几千年来，黄金在医学上一直扮演着重要的角色。最近，人们对金络合物治疗药物的兴趣重新焕发生机，关于先导化合物Auranofin的几项正在进行的临床试验就是例证。然而，已批准的黄金药物的最大挑战与它们的化学和代谢稳定性不足以及它们的低选择性有关。本项目旨在设计新的金抗癌金属药物，以克服这些重大限制。新试剂含有核苷和碳水化合物部分，以促进靶向和提高抗增殖能力。该项目将在德国和俄罗斯科学家之间以双边合作的形式进行。将利用双方互补的研究专长，对新化合物进行详细的化学和生物调查。选定的有希望的主要候选者将在体内进行进一步的研究，并为未来可能转化为应用提供基础。

Gold has been playing an important role in medicine tracing back thousands of years. Recently, the interest in gold complexes therapeutic drugs has come to new life as exemplified by several ongoing clinical trials on the lead compound Auranofin. However, the biggest challenges of the approved gold drugs are related to their insufficient chemical and metabolic stability as well as to their low selectivity. This project aims at the design of new gold anticancer metallodrugs, which could overcome these major limitations. The new agents contain nucleoside and carbohydrate moieties to facilitate targeting and to improve the antiproliferative potency. The project will be performed in form of a bilateral collaboration between German and Russian scientists. The new compounds will be subjected to a detailed chemical and biological investigation making use of the complementary research expertise of both partners. Selected promising lead candidates will be studied further in-vivo and provide the basis for a possible future translation into application.