Synthesis and migrastatic activity of cytochalasin analogues lacking a macrocyclic moiety.

ABSTRACT: 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, wi

SUBMITTER: Formanek B 

PROVIDER: S-EPMC10809383 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature