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  • Title: Synthesis of pyrrolo[3,2-h]quinolinones with good photochemotherapeutic activity and no DNA damage.
    Author: Barraja P, Caracausi L, Diana P, Carbone A, Montalbano A, Cirrincione G, Brun P, Palù G, Castagliuolo I, Dall'acqua F, Vedaldi D, Salvador A.
    Journal: Bioorg Med Chem; 2010 Jul 01; 18(13):4830-43. PubMed ID: 20627596.
    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.
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