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ToolsSulik, Michal, Otto-Ślusarczyk, Dagmara, Steverding, Dietmar, Struga, Marta and Huczyński, Adam (2025) Antiproliferative and trypanocidal activity of ivermectin bioconjugates. ACS Omega. ISSN 2470-1343
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Abstract
Ivermectin (IVR), whose discovery has been Nobel-Prize-honored, is a 16-membered macrocyclic lactone used in medicine as an extremely effective and safe antiparasitic drug. In recent years, interest in this compound has grown due to its potential effectiveness in killing various types of cancer cells. However, research on the anticancer activity of IVR derivatives is limited. Additionally, the growing problem of drug resistance raises concerns about the effectiveness of this drug in the treatment of parasitic diseases. Therefore, in this work, we provide a detailed description of the synthesis of ten new IVR bioconjugates with compounds exhibiting high anticancer and/or antimicrobial activity. We also assess the effectiveness of these hybrids in killing Trypanosoma brucei brucei a protozoan parasite that causes African trypanosomiasis, as well as their anticancer activity toward various cancer cell lines. Many of the newly synthesized conjugates exhibited higher biological activity than their respective parent compounds as well as increased selectivity indices. The IVR conjugate with artesunate (compound 16) appears particularly interesting, as it proved not only to be several times more active than the parent compounds but also showed no toxicity toward a reference cell line, indicating its potential as a therapeutic agent.
| Item Type: | Article |
|---|---|
| Additional Information: | Data Availability Statement: The data underlying this study are available in the published article and its Supporting Information. |
| Uncontrolled Keywords: | sdg 3 - good health and well-being ,/dk/atira/pure/sustainabledevelopmentgoals/good_health_and_well_being |
| Faculty \ School: | Faculty of Medicine and Health Sciences > Norwich Medical School |
| UEA Research Groups: | Faculty of Medicine and Health Sciences > Research Groups > Gastroenterology and Gut Biology |
| Related URLs: | |
| Depositing User: | LivePure Connector |
| Date Deposited: | 16 Jun 2025 12:30 |
| Last Modified: | 26 Jun 2025 10:30 |
| URI: | https://ueaeprints.uea.ac.uk/id/eprint/99563 |
| DOI: | 10.1021/acsomega.5c02998 |
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