Metallo Nucleosides: Gold Complexes with Antimetabolite Ligands

• Applicant: Professor Dr. Ingo Ott
• Subject Area: Biological and Biomimetic Chemistry ; Pharmacy
• Term: from 2019 to 2023
• Project identifier: Deutsche Forschungsgemeinschaft (DFG) - Project number 409903581

• Final Report Year: 2024

Final Report Abstract

The project aimed at the synthesis, characterisation and detailed biological evaluation of gold complexes with antimetabolite ligands. In such compounds a gold moiety is connected with a nucleoside by a glucose phosphite based partial structure, providing the conjugates with dual targeting properties. While the gold center triggers known effects of gold complexes, such as inhibition of the redox enzyme thioredoxin reductase, the nucleoside will lead to DNA interactions. The combined effect of the two bioactive centers is expected to cause an efficient reduction of tumor cell proliferation, making the complexes interesting novel anticancer drug candidates. The project has been performed as a joint collaboration between scientists from Technische Universität Braunschweig and Moscow State University. As a consequence of the suspension of the German-Russian collaborations by Technische Universität Braunschweig and the DFG after the Russian attack on Ukraine, the project could not be completed.

Publications

• Metallodrug Profiling against SARS‐CoV‐2 Target Proteins Identifies Highly Potent Inhibitors of the S/ACE2 interaction and the Papain‐like Protease PLpro. Chemistry – A European Journal, 27(71), 17928-17940.
  Gil‐Moles, Maria; Türck, Sebastian; Basu, Uttara; Pettenuzzo, Andrea; Bhattacharya, Saurav; Rajan, Ananthu; Ma, Xiang; Büssing, Rolf; Wölker, Jessica; Burmeister, Hilke; Hoffmeister, Henrik; Schneeberg, Pia; Prause, Andre; Lippmann, Petra; Kusi‐Nimarko, Josephine; Hassell‐Hart, Storm; McGown, Andrew; Guest, Daniel; Lin, Yan ... & Ott, Ingo