Heteroanalogues of angelicin, pyrrolo[3,2-h]quinazolines, were synthesized with the aim of obtaining new potent photochemotherapeutic agents. Many derivatives caused a significant decrease in cell proliferation in several human tumor cell lines after irradiation with UVA light (GI50=15.2–0.2 mm). Their phototoxicity effected apoptosis in Jurkat cells with the involvement of mitochondria (as determined by the loss of mitochondrial membrane potential and production of reactive oxygen species) and lysosomes. The phototoxicity of these compounds could be explained by lipid peroxidation.

Barraja, P., Caracausi, L., Diana, P., Montalbano, A., Carbone, A., Salvador, A., et al. (2011). Pyrrolo[3,2-h]quinazolines as Photochemotherapeutic Agents. CHEMMEDCHEM, 6, 1238-1248 [10.1002/CMDC.201100085].

Pyrrolo[3,2-h]quinazolines as Photochemotherapeutic Agents

BARRAJA, Paola;DIANA, Patrizia;MONTALBANO, Alessandra;CARBONE, Anna;CIRRINCIONE, Girolamo
2011-01-01

Abstract

Heteroanalogues of angelicin, pyrrolo[3,2-h]quinazolines, were synthesized with the aim of obtaining new potent photochemotherapeutic agents. Many derivatives caused a significant decrease in cell proliferation in several human tumor cell lines after irradiation with UVA light (GI50=15.2–0.2 mm). Their phototoxicity effected apoptosis in Jurkat cells with the involvement of mitochondria (as determined by the loss of mitochondrial membrane potential and production of reactive oxygen species) and lysosomes. The phototoxicity of these compounds could be explained by lipid peroxidation.
2011
Settore CHIM/08 - Chimica Farmaceutica
Barraja, P., Caracausi, L., Diana, P., Montalbano, A., Carbone, A., Salvador, A., et al. (2011). Pyrrolo[3,2-h]quinazolines as Photochemotherapeutic Agents. CHEMMEDCHEM, 6, 1238-1248 [10.1002/CMDC.201100085].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/55069
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