6533b7ddfe1ef96bd1275535
RESEARCH PRODUCT
Pyrazolo[3,4-h]quinolines promising photosensitizing agents in the treatment of cancer.
Paola BarrajaDaniela VedaldiPaola BrunAlessia SalvadorAnna CarboneVirginia SpanòPatrizia DianaBarbara ParrinoAlessandra MontalbanoGirolamo Cirrincionesubject
Programmed cell deathPhotodynamic therapy; Antiproliferative activity; Photosensitizing agents; Reactive oxygen species; PUVA therapyPUVA therapymedicine.medical_treatmentPhotodynamic therapyAntineoplastic AgentsAntiproliferative activityPhotodynamic therapy Antiproliferative activity Photosensitizing agents Reactive oxygen species PUVA therapyMitochondrionPhotodynamic therapychemistry.chemical_compoundStructure-Activity RelationshipAngelicinCell Line TumorDrug DiscoverymedicineStructure–activity relationshipHumansCell ProliferationPharmacologyPhotosensitizing AgentsDose-Response Relationship DrugMolecular StructureCell growthOrganic ChemistryGeneral MedicinePhotosensitizing AgentSettore CHIM/08 - Chimica FarmaceuticaFurocoumarinsBiochemistrychemistryQuinolinesPyrazolesDrug Screening Assays AntitumorReactive oxygen speciesdescription
A new series of pyrazolo[3,4-h]quinolines, heteroanalogues of angelicin was conveniently prepared with a broad substitution pattern. A large number of derivatives was obtained and the cellular photocytotoxicity was evaluated in vitro against 5 different human tumor cell lines with GI50 values reaching the nanomolar level (14.52e0.04 mM). Selected compounds were able to photoinduce a massive cell death with the involvement of mitochondria. Their photodamage cellular targets were proteins and lipids and they did not cause any kind of DNA photodamage. This latter event is of considerable importance in the modulation of long term side effects, generally associated with the use of classical furocoumarins.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2015-01-01 | European journal of medicinal chemistry |