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.
Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Apoptosis / drug effects
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Cell Line, Tumor
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Drug Screening Assays, Antitumor
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Furocoumarins / chemical synthesis
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Furocoumarins / chemistry
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Furocoumarins / toxicity
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Humans
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Photosensitizing Agents / chemical synthesis
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Photosensitizing Agents / chemistry*
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Photosensitizing Agents / toxicity
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Pyrroles / chemical synthesis
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Pyrroles / chemistry*
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Pyrroles / toxicity
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Quinolines / chemical synthesis
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Quinolines / chemistry*
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Quinolines / toxicity
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Reactive Oxygen Species / metabolism
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Structure-Activity Relationship
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Ultraviolet Rays
Substances
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Furocoumarins
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Photosensitizing Agents
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Pyrroles
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Quinolines
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Reactive Oxygen Species
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pyrroloquinoline
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angelicin