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Pyrrolo[3,2‐ h ]quinazolines as Photochemotherapeutic Agents
Author(s) -
Barraja Paola,
Caracausi Libero,
Diana Patrizia,
Montalbano Alessandra,
Carbone Anna,
Salvador Alessia,
Brun Paola,
Castagliuolo Ignazio,
Tisi Silvia,
Dall'Acqua Francesco,
Vedaldi Daniela,
Cirrincione Girolamo
Publication year - 2011
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201100085
Subject(s) - phototoxicity , jurkat cells , apoptosis , reactive oxygen species , chemistry , mitochondrion , lipid peroxidation , cell culture , cell growth , membrane potential , photosensitizer , inner mitochondrial membrane , cell , biochemistry , pharmacology , microbiology and biotechnology , biophysics , oxidative stress , in vitro , biology , immunology , photochemistry , t cell , genetics , immune system
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 μ M ). 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.