SYNTHESIS OF PYRROLO[3,2-H]QUINOLINONES WITH GOOD PHOTOCHEMOTHERAPEUTIC ACTIVITY AND NO DNA DAMAGE
- Autori: BARRAJA, P; CARACAUSI, L; DIANA, P; CARBONE, A; MONTALBANO, A; CIRRINCIONE, G; BRUN, P; PALU', G; CASTAGLIUOLO, I; DALL'ACQUA, F; VEDALDI, D; SALVADOR, A
- Anno di pubblicazione: 2010
- Tipologia: Articolo in rivista (Articolo in rivista)
- Parole Chiave: PYRROLO[3,2-H]QUINOLINONES; ANGELICIN HETEROANALOGUES; PHOTOCHEMOTHERAPY; PHOTOTOXICITY
- OA Link: http://hdl.handle.net/10447/51294
Abstract
In the search for new photochemotherapeutic agents, a series of derivatives of the ring system pyrrolo[3,2-h]quinoline—bioisosters of the angular furocoumarin angelicin—were synthesized through a four-step synthetic approach, in reasonable overall yields. Eight of the synthesized derivatives showed a remarkable phototoxicity against a panel of four human tumor cell lines and a great dose UV-A dependence, reaching IC50 values at submicromolar level. The mode of cellular death photoinduced by pyrrolo[3,2-h]quinolines was evaluated through a series of flow cytometric analysis and other tests were performed to clarify their mechanism of action.