6533b828fe1ef96bd128859a

RESEARCH PRODUCT

SYNTHESIS AND PHOTOCHEMIOTHERAPEUTIC ACTIVITY OF THIOPYRANO[2,3-E]INDOL-2-ONES

Silvia DisaròLaura SciabicaGaetano DattoloAntonino LauriaPaola BarrajaFrancesco Dall'acquaGirolamo CirrincioneGiuseppe BassoAnna Maria AlmericoGiampietro ViolaPatrizia DianaAlessandra Montalbano

subject

IndolesCell SurvivalUltraviolet RaysStereochemistryClinical BiochemistrySubstituentPharmaceutical ScienceHL-60 CellsRing (chemistry)BiochemistryChemical synthesischemistry.chemical_compoundCell Line TumorDrug DiscoveryThiolactoneHumansPhotosensitizerCytotoxicityMolecular BiologyIC50PyransPyrrolePhotosensitizing AgentsChemistryOrganic ChemistryDNA NeoplasmCombinatorial chemistrySettore CHIM/08 - Chimica FarmaceuticaThiopyrano-indoles Photochemotherapeutic activity Apoptosis inductionPhotochemotherapyMolecular MedicineCell Division

description

A series of derivatives of the new ring system thiopyrano[2,3-e]indol-2-one was prepared with the aim of obtaining new photochemotherapeutic drugs. Biological screenings were performed on this new class of photoactivable drugs and a strong antiproliferative effect was observed upon irradiation with UVA light. The compound bearing a methyl substituent at the pyrrole nitrogen resulted as the most interesting showing IC50 in the nanomolar range.

yearjournalcountryeditionlanguage
2004-10-28
10.1016/j.bmcl.2005.03.016http://hdl.handle.net/10447/21203