Research Projects
Dexrazoxane |
||
|
J. Med. Chem. 2021 |
Dexrazoxane is a clinically used drug to prevent anthracycline cardiotoxicity. We are investigating the structure-activity relationships of dexrazoxane analogues with a focus on their ability to protect the heart against anthracycline cardiotoxicity. An important part of this is to investigate the mechanisms responsible for the cardioprotective efficacy of dexrazoxane and its analogs, particularly their ability to catalytically inhibit topoisomerase II. | |
Topoisomerase II Inhibitors |
||
|
Nat. Commun. 2025 |
Our research focuses on the development of topoisomerase II inhibitors and the investigation of their structure–activity relationships. Particular emphasis is placed on designing compounds that selectively target individual topoisomerase II isoforms. These selective TOP2β inhibitors are being explored as potential cardioprotective agents against anthracycline-induced cardiotoxicity and as valuable tools for studying the biological role of TOP2β. Using a rational drug design approach, we developed topobexin, a novel TOP2β-selective inhibitor that interacts with amino acid residues distinguishing TOP2A from TOP2B. Topobexin provides greater selectivity and inhibitory potency than dexrazoxane and has demonstrated significant protection against chronic anthracycline-induced cardiotoxicity in animal models. Ongoing research is focused on the intensive optimization of this compound series through detailed structure–activity relationship studies. |
|
Anti-Tuberculosis Agents |
||
|
J. Med. Chem. 2024 |
We focus on the development and study of structure-activity relationships of different structural types of potential anti-tuberculosis drugs. In one part of our research we focus on nitro compounds, mainly with a 3,5-dinitrophenyl fragment in the molecule. Depending on the structure, these compounds are potent inhibitors of DprE1 or act by a deazaflavin-dependent nitroreductase-mediated mechanisms. Other groups studied are mainly heterocyclic compounds acting by different mechanisms of anti-TB action. |
|
