RSC Medicinal Chemistry · 2023 · 10 citations · 50 references
PharmacyMedicinal ChemistryPharmacologyCytoskeletonDrug DiscoveryStructure-activity RelationshipsActin FilamentsActin PolymerizationEnzyme InhibitionMacrocycle SynthesisStructure-activity Relationship AnalysisActin Polymerization ControlActin Polymerization InhibitorsChemical Synthesis Of AnaloguesConcentrationCytoskeletal Drug DiscoveryMacrocyclic Ligands
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.
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