6533b85dfe1ef96bd12bdea0

RESEARCH PRODUCT

Stilbene-based anticancer agents: Resveratrol analogues active toward HL60 leukemic cells wit a non-specific phase mechanism

Nicola GebbiaAntonietta Di CristinaRiccardo BaruchelloEnrico AielloFrancesco DieliMarco EleopraPaolo MarchettiFrancesco Paolo InvidiataMarinella RobertiLucia CrostaManlio TolomeoDaniele SimoniStefania GrimaudoStefania Aiello

subject

AntimonyHL60Clinical BiochemistryPharmaceutical ScienceAntineoplastic AgentsHL-60 CellsResveratrolBiochemistryStructure-Activity Relationshipchemistry.chemical_compoundStilbenesDrug DiscoverymedicineHumansStructure–activity relationshipMolecular BiologyS phaseCell ProliferationMolecular StructureOrganic ChemistryCell cycleMechanism of actionchemistryBiochemistryAnticancer agentResveratrolCell cultureApoptosisResveratrol analogueCell cycle analysisMolecular Medicinemedicine.symptom

description

Several stilbenes, related to known resveratrol, have been synthesized and tested for their anticancer effect on HL60 leukemia cell line, taking particular care of the cell cycle analysis. The most potent compound was the known (Z)-3,4',5-trimethoxystilbene (6b) which was active as apoptotic agent at 0.24 microM. Differently from other stilbenes (including resveratrol) that induced a prevalent recruitment of cells in S phase of cell cycle, we found a peculiar behavior of 6b that caused a decrease of cells in all phases of cell cycle (G0-G1, S, and G2-M) and a proportional increase of apoptotic cells. The potent pro-apoptotic activity shown by compound 6b and its effects on cell cycle make this compound of great interest for further investigations.

http://hdl.handle.net/11392/1209331