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Updated: Jun 2, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Pyrrolo[3,2-h]quinazolines as photochemotherapeutic agents
Paola Barraja1, Libero Caracausi, Patrizia Diana
1Dipartimento di Scienze e Tecnologie Molecolari e Biomolecolari, Sezione Chimica Farmaceutica e Biologica, Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy.
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 (GI(50) =15.2-0.2 μM). 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.
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