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HPMA-based polymer conjugates for repurposed drug mebendazole and other imidazole-based therapeutics
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SYSNO ASEP 0545100 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název HPMA-based polymer conjugates for repurposed drug mebendazole and other imidazole-based therapeutics Tvůrce(i) Studenovský, Martin (UMCH-V) RID, ORCID
Rumlerová, Anna (UMCH-V)
Kostka, Libor (UMCH-V) RID, ORCID
Etrych, Tomáš (UMCH-V) RID, ORCIDČíslo článku 2530 Zdroj.dok. Polymers. - : MDPI
Roč. 13, č. 15 (2021)Poč.str. 14 s. Jazyk dok. eng - angličtina Země vyd. CH - Švýcarsko Klíč. slova mebendazole ; drug delivery ; drug repurposing Vědní obor RIV CD - Makromolekulární chemie Obor OECD Polymer science CEP GA19-01417S GA ČR - Grantová agentura ČR GA19-05649S GA ČR - Grantová agentura ČR LTAUSA18083 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy Způsob publikování Open access Institucionální podpora UMCH-V - RVO:61389013 UT WOS 000682200100001 EID SCOPUS 85111635782 DOI 10.3390/polym13152530 Anotace 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. Pracoviště Ústav makromolekulární chemie Kontakt Eva Čechová, cechova@imc.cas.cz ; Tel.: 296 809 358 Rok sběru 2022 Elektronická adresa https://www.mdpi.com/2073-4360/13/15/2530
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