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

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61389013%3A_____%2F21%3A00545100" target="_blank" >RIV/61389013:_____/21:00545100 - isvavai.cz</a>

  • Result on the web

    <a href="https://www.mdpi.com/2073-4360/13/15/2530" target="_blank" >https://www.mdpi.com/2073-4360/13/15/2530</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.3390/polym13152530" target="_blank" >10.3390/polym13152530</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

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

  • Original language description

    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.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • OECD FORD branch

    10404 - Polymer science

Result continuities

  • Project

    Result was created during the realization of more than one project. More information in the Projects tab.

  • Continuities

    I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Others

  • Publication year

    2021

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    Polymers

  • ISSN

    2073-4360

  • e-ISSN

    2073-4360

  • Volume of the periodical

    13

  • Issue of the periodical within the volume

    15

  • Country of publishing house

    CH - SWITZERLAND

  • Number of pages

    14

  • Pages from-to

    2530

  • UT code for WoS article

    000682200100001

  • EID of the result in the Scopus database

    2-s2.0-85111635782