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

Bioorganic & Medicinal Chemistry
Paola BarrajaAlessia Salvador

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.

References

Jul 30, 1991·Biochimica Et Biophysica Acta·P MorlièreL Dubertret
Mar 28, 2003·Photochemical & Photobiological Sciences : Official Journal of the European Photochemistry Association and the European Society for Photobiology·Sergio Caffieri

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Citations

Mar 15, 2015·European Journal of Medicinal Chemistry·Barbara ParrinoNadia Zaffaroni
Sep 2, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Barbara ParrinoAlessandra Montalbano
Aug 22, 2015·European Journal of Medicinal Chemistry·Virginia SpanòPaola Barraja
Apr 1, 2014·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Alessia SalvadorStefano Dall'Acqua
Mar 23, 2013·Journal of Photochemistry and Photobiology. B, Biology·Alessia SalvadorRoberto Gambari
Mar 18, 2015·European Journal of Medicinal Chemistry·Barbara ParrinoPatrizia Diana
Feb 4, 2014·European Journal of Medicinal Chemistry·Virginia SpanòPaola Barraja
Jul 19, 2016·Journal of Medicinal Chemistry·Virginia SpanòNadia Zaffaroni
Sep 20, 2016·European Journal of Medicinal Chemistry·Virginia SpanòPaola Barraja
Aug 24, 2012·ChemMedChem·Paola BarrajaGirolamo Cirrincione
May 17, 2011·ChemMedChem·Paola BarrajaGirolamo Cirrincione
Jan 6, 2021·European Journal of Medicinal Chemistry·Virginia SpanòPaola Barraja
Mar 4, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Virginia SpanòPaola Barraja

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