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HPMA-based polymer conjugates for repurposed drug mebendazole and other imidazole-based therapeutics

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    SYSNO ASEP0545100
    Document TypeJ - Journal Article
    R&D Document TypeJournal Article
    Subsidiary JČlánek ve WOS
    TitleHPMA-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, ORCID
    Article number2530
    Source TitlePolymers. - : MDPI
    Roč. 13, č. 15 (2021)
    Number of pages14 s.
    Languageeng - English
    CountryCH - Switzerland
    Keywordsmebendazole ; drug delivery ; drug repurposing
    Subject RIVCD - Macromolecular Chemistry
    OECD categoryPolymer science
    R&D ProjectsGA19-01417S 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 publishingOpen access
    Institutional supportUMCH-V - RVO:61389013
    UT WOS000682200100001
    EID SCOPUS85111635782
    DOI10.3390/polym13152530
    AnnotationRecently, 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.
    WorkplaceInstitute of Macromolecular Chemistry
    ContactEva Čechová, cechova@imc.cas.cz ; Tel.: 296 809 358
    Year of Publishing2022
    Electronic addresshttps://www.mdpi.com/2073-4360/13/15/2530
Number of the records: 1  

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