6533b7d0fe1ef96bd125add2

RESEARCH PRODUCT

Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-N,N-dimethylamino benzo[b]furan derivatives as inhibitors of tubulin polymerization

Taradas SarkarOlga Cruz-lopezRomeo RomagnoliRoberto GambariManlio TolomeoErnest HamelMaria Rosaria PipitoneMaria Dora CarrionPier Giovanni BaraldiAntonietta Di CristinaLampronti IlariaStefania GrimaudoJan BalzariniAndrea BrancaleRoberto SalettiCarlota Lopez Cara

subject

StereochemistryClinical BiochemistryPharmaceutical Sciencemacromolecular substancesAntimitotic AgentsBiochemistryChemical synthesisArticlechemistry.chemical_compoundInhibitory Concentration 50MiceStructure-Activity RelationshipMicrotubuleFuranCell Line TumorDrug Discoverypolycyclic compoundsTumor Cells CulturedStructure–activity relationshipAnimalsHumansMolecular BiologyBenzofuransCell ProliferationCombretastatin A-4biologyTubulin ModulatorsOrganic ChemistryTubulin ModulatorsTubulinchemistrybiology.proteinMolecular MedicineBioisostereProtein Binding

description

Molecules that target microtubules have an important role in the treatment of cancer. A new class of inhibitors of tubulin polymerization based on the 2-(3,4,5-trimethoxybenzoyl)-2-dimethylamino-benzo[b]furan molecular skeleton was synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, and cell cycle effects. The most promising compound in this series was 2-(3,4,5-trimethoxybenzoyl)-3-dimethylamino-6-methoxy-benzo[b]furan, which inhibits cancer cell growth at nanomolar concentrations and interacts strongly with tubulin by binding to the colchicine site.

yearjournalcountryeditionlanguage
2008-09-01
http://hdl.handle.net/10447/34019