Počet záznamů: 1  

Synthesis and migrastatic activity of cytochalasin analogues lacking a macrocyclic moiety

  1. 1.
    SYSNO ASEP0581608
    Druh ASEPJ - Článek v odborném periodiku
    Zařazení RIVJ - Článek v odborném periodiku
    Poddruh JČlánek ve WOS
    NázevSynthesis and migrastatic activity of cytochalasin analogues lacking a macrocyclic moiety
    Tvůrce(i) Formánek, B. (CZ)
    Dupommier, D. (CZ)
    Volfová, T. (CZ)
    Rimpelová, S. (CZ)
    Škarková, A. (CZ)
    Herciková, J. (CZ)
    Rösel, D. (CZ)
    Brábek, J. (CZ)
    Perlíková, Pavla (UOCHB-X) RID, ORCID
    Zdroj.dok.RSC MEDICINAL CHEMISTRY. - : Royal Society of Chemistry
    Roč. 15, č. 1 (2024), s. 322-343
    Poč.str.22 s.
    Jazyk dok.eng - angličtina
    Země vyd.GB - Velká Británie
    Klíč. slovaactin polymerization ; cellular structures ; alkyl halides
    Obor OECDOrganic chemistry
    CEPLX22NPO5102 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy
    Způsob publikováníOpen access
    Institucionální podporaUOCHB-X - RVO:61388963
    UT WOS001127188400001
    EID SCOPUS85180612986
    DOI10.1039/d3md00535f
    AnotaceCytochalasans are known as inhibitors of actin polymerization and for their cytotoxic and migrastatic activity. In this study, we synthesized a series of cytochalasin derivatives that lack a macrocyclic moiety, a structural element traditionally considered essential for their biological activity. We focused on substituting the macrocycle with simple aryl-containing sidechains, and we have also synthesized compounds with different substitution patterns on the cytochalasin core. The cytochalasin analogues were screened for their migrastatic and cytotoxic activity. Compound 24 which shares the substitution pattern with natural cytochalasins B and D exhibited not only significant in vitro migrastatic activity towards BLM cells but also demonstrated inhibition of actin polymerization, with no cytotoxic effect observed at 50 mu M concentration. Our results demonstrate that even compounds lacking the macrocyclic moiety can exhibit biological activities, albeit less pronounced than those of natural cytochalasins. However, our findings emphasize the pivotal role of substituting the core structure in switching between migrastatic activity and cytotoxicity. These findings hold significant promise for further development of easily accessible cytochalasan analogues as novel migrastatic agents.
    PracovištěÚstav organické chemie a biochemie
    Kontaktasep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Jana Procházková, Tel.: 220 183 418
    Rok sběru2025
    Elektronická adresahttps://doi.org/10.1039/D3MD00535F
Počet záznamů: 1  

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