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

被引:51
作者
Barraja, Paola [1 ]
Caracausi, Libero [1 ]
Diana, Patrizia [1 ]
Montalbano, Alessandra [1 ,2 ]
Carbone, Anna [1 ]
Salvador, Alessia
Brun, Paola [3 ]
Castagliuolo, Ignazio [3 ]
Tisi, Silvia [2 ]
Dall'Acqua, Francesco [2 ]
Vedaldi, Daniela [2 ]
Cirrincione, Girolamo [1 ]
机构
[1] Univ Palermo, Sez Chim Farmaceut & Biol, Dipartimento Sci & Tecnol Mol & Biomol, I-90123 Palermo, Italy
[2] Univ Padua, Dipartimento Sci Farmaceut, I-35131 Padua, Italy
[3] Univ Padua, Dipartimento Istol Microbiol & Biotecnol Med, I-35121 Padua, Italy
关键词
angelicin heteroanalogues; antitumor agents; apoptosis; photochemotherapeutic agents; pyrrolo[3,2-h]quinazolines; CULTURED HUMAN FIBROBLASTS; ANTITUMOR AGENTS; APOPTOSIS; DERIVATIVES; ASSAY; HETEROCYCLES; ANALOGS;
D O I
10.1002/cmdc.201100085
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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 mu 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.
引用
收藏
页码:1238 / 1248
页数:11
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