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HPMA-based polymer conjugates for repurposed drug mebendazole and other imidazole-based therapeutics
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SYSNO ASEP 0545100 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title HPMA-based polymer conjugates for repurposed drug mebendazole and other imidazole-based therapeutics Author(s) Studenovský, Martin (UMCH-V) RID, ORCID
Rumlerová, Anna (UMCH-V)
Kostka, Libor (UMCH-V) RID, ORCID
Etrych, Tomáš (UMCH-V) RID, ORCIDArticle number 2530 Source Title Polymers. - : MDPI
Roč. 13, č. 15 (2021)Number of pages 14 s. Language eng - English Country CH - Switzerland Keywords mebendazole ; drug delivery ; drug repurposing Subject RIV CD - Macromolecular Chemistry OECD category Polymer science R&D Projects GA19-01417S GA ČR - Czech Science Foundation (CSF) GA19-05649S GA ČR - Czech Science Foundation (CSF) LTAUSA18083 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) Method of publishing Open access Institutional support UMCH-V - RVO:61389013 UT WOS 000682200100001 EID SCOPUS 85111635782 DOI 10.3390/polym13152530 Annotation Recently, the antitumor potential of benzimidazole anthelmintics, such as mebendazole and its analogues, have been reported to have minimal side effects, in addition to their well-known anti-parasitic abilities. However, their administration is strongly limited owing to their extremely poor solubility, which highly depletes their overall bioavailability. This study describes the design, synthesis, and physico-chemical properties of polymer-mebendazole nanomedicines for drug repurposing in cancer therapy. The conjugation of mebendazole to water-soluble and biocompatible polymer carrier was carried out via biodegradable bond, relying on the hydrolytic action of lysosomal hydrolases for mebendazole release inside the tumor cells. Five low-molecular-weight mebendazole derivatives, differing in their inner structure, and two polymer conjugates differing in their linker structure, were synthesized. The overall synthetic strategy was designed to enable the modification and polymer conjugation of most benzimidazole-based anthelmintics, such as albendazole, fenbendazole or albendazole, besides the mebendazole. Furthermore, the described methodology may be suitable for conjugation of other biologically active compounds with a heterocyclic N-H group in their molecules. Workplace Institute of Macromolecular Chemistry Contact Eva Čechová, cechova@imc.cas.cz ; Tel.: 296 809 358 Year of Publishing 2022 Electronic address https://www.mdpi.com/2073-4360/13/15/2530
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