6533b85cfe1ef96bd12bd4d1

RESEARCH PRODUCT

Pyrrolo[3,2-h]quinazolines as Photochemotherapeutic Agents

Anna CarbonePatrizia DianaSilvia TisiIgnazio CastagliuoloLibero CaracausiGirolamo CirrincioneAlessia SalvadorFrancesco Dall'acquaPaola BarrajaDaniela VedaldiAlessandra MontalbanoPaola Brun

subject

Pyrrolo[3; 2-h]quinazolines; Angelicin; Photochemotherapeutic AgentsAngelicinUltraviolet RaysApoptosisMitochondrion2-h]quinazolinesBiochemistryJurkat cellsLipid peroxidationStructure-Activity Relationshipchemistry.chemical_compoundAngelicinCell Line TumorFurocoumarinsPhotochemotherapeutic AgentsDrug DiscoveryHumansPyrrolo[32-h]quinazolinePyrrolesPyrrolo[3General Pharmacology Toxicology and PharmaceuticsPharmacologychemistry.chemical_classificationReactive oxygen speciesPhotosensitizing AgentsOrganic ChemistrySettore CHIM/08 - Chimica FarmaceuticachemistryBiochemistryApoptosisCell cultureQuinolinesMolecular MedicineDrug Screening Assays AntitumorReactive Oxygen SpeciesPhototoxicity

description

Heteroanalogues of angelicin, pyrrolo[3,2-h]quinazolines, were synthesized with the aim of obtaining new potent photochemotherapeutic agents. Many derivatives caused a significant decrease in cell proliferation in several human tumor cell lines after irradiation with UVA light (GI(50) =15.2-0.2 μM). Their phototoxicity effected apoptosis in Jurkat cells with the involvement of mitochondria (as determined by the loss of mitochondrial membrane potential and production of reactive oxygen species) and lysosomes. The phototoxicity of these compounds could be explained by lipid peroxidation.

yearjournalcountryeditionlanguage
2011-01-01ChemMedChem
https://doi.org/10.1002/cmdc.201100085