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Synthesis and migrastatic activity of cytochalasin analogues lacking a macrocyclic moiety

Bedřich Formánek, Dorian Dupommier, Tereza Volfová, Silvie Rimpelová, Aneta Škarková, Jana Herciková, Daniel Rösel, Jan Brábek, Pavla Perlíková

2023RSC Medicinal Chemistry10 citationsDOIOpen Access PDF

Abstract

migrastatic activity towards BLM cells but also demonstrated inhibition of actin polymerization, with no cytotoxic effect observed at 50 μM 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.

Topics & Concepts

MoietyCytochalasinChemistryCytochalasin BCytotoxicityCytochalasin DIn vitroStereochemistryBiological activityCytotoxic T cellActinPolymerizationBiochemistryCytoskeletonCellOrganic chemistryPolymerInnovative Microfluidic and Catalytic Techniques InnovationAdvanced Fluorescence Microscopy TechniquesAdvanced Polymer Synthesis and Characterization
Synthesis and migrastatic activity of cytochalasin analogues lacking a macrocyclic moiety | Litcius