2. Academic Validation
  3. Synthesis of pyrrolo[3,2-h]quinolinones with good photochemotherapeutic activity and no DNA damage

Synthesis of pyrrolo[3,2-h]quinolinones with good photochemotherapeutic activity and no DNA damage

  • Bioorg Med Chem. 2010 Jul 1;18(13):4830-43. doi: 10.1016/j.bmc.2010.04.080.
Paola Barraja 1,  Libero Caracausi,  Patrizia Diana,  Anna Carbone,  Alessandra Montalbano,  Girolamo Cirrincione,  Paola Brun,  Giorgio Palù,  Ignazio Castagliuolo,  Francesco Dall'acqua,  Daniela Vedaldi,  Alessia Salvador
Affiliations

Affiliation

  • 1 Dipartimento Farmacochimico, Tossicologico e Biologico, Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy.
PMID: 20627596 DOI: 10.1016/j.bmc.2010.04.080
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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