Pyrrolo[3,4-h]quinolinones a new class of photochemotherapeutic agents

Paola Barraja, Alessandra Montalbano, Patrizia Diana, Girolamo Cirrincione, Anna Carbone, Alessia Salvador, Daniela Vedaldi, Francesco Dall'Acqua, Giampietro Viola, Giuseppe Basso

Risultato della ricerca: Articlepeer review

37 Citazioni (Scopus)

Abstract

Pyrrolo[3,4-h]quinolin-2-ones were synthesized as nitrogen isosters of the angular furocoumarin angelicin, with the aim of obtaining new photochemotherapeutic agents with increased antiproliferative activity and lower undesired toxic effects. A versatile synthetic pathway was approached to allow the isolation of derivatives of the new ring system with a good substitution pattern on the pyrrole moiety. Photobiological screenings of the new compounds revealed a potent phototoxic effect and a great UVA dosedependence, reaching IC50 values at submicromolar level. The induced cellular photocytotoxicity was related to apoptosis with the involvement of mitochondria and lysosomes, alteration of cell cycle profile and membrane lipid peroxidation.
Lingua originaleEnglish
pagine (da-a)2326-2341
Numero di pagine16
RivistaBIOORGANIC & MEDICINAL CHEMISTRY
Volume19
Stato di pubblicazionePublished - 2011

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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