Počet záznamů: 1
Synthesis and migrastatic activity of cytochalasin analogues lacking a macrocyclic moiety
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SYSNO ASEP 0581608 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Synthesis 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, ORCIDZdroj.dok. RSC MEDICINAL CHEMISTRY. - : Royal Society of Chemistry
Roč. 15, č. 1 (2024), s. 322-343Poč.str. 22 s. Jazyk dok. eng - angličtina Země vyd. GB - Velká Británie Klíč. slova actin polymerization ; cellular structures ; alkyl halides Obor OECD Organic chemistry CEP LX22NPO5102 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy Způsob publikování Open access Institucionální podpora UOCHB-X - RVO:61388963 UT WOS 001127188400001 EID SCOPUS 85180612986 DOI 10.1039/d3md00535f Anotace Cytochalasans 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. Pracoviště Ústav organické chemie a biochemie Kontakt asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Jana Procházková, Tel.: 220 183 418 Rok sběru 2025 Elektronická adresa https://doi.org/10.1039/D3MD00535F
Počet záznamů: 1