期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 53, 期 -, 页码 264-274出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.04.008
关键词
Antitumor agents; Cell cycle; beta-Lapachone; Naphthoquinone; Structure-activity relationships
资金
- European Social Fund (FEDER)
- Spanish Instituto de Salud Carlos III [PI11/00840]
- Spanish MSC (RTICC) [RD06/0020/1046, RD06/0020/0041]
- Canary Islands ACIISI [PI 2007/021]
- Canary Islands FUNCIS [PI 43/09]
- Consejo Nacional de lnvestigaciones Cientificas y Tecnicas (CONICET) [PIP 0447]
- Universidad de Buenos Aires (UBACyT) [20020090200697]
- ACIISI [SE-10/19]
In this study, we describe the synthesis of a series of alpha- and beta-lapachone containing hydroxyl or methoxyl groups on the benzene ring, by means of the selective acid promoted cyclization of the appropriate lapachol analog. The evaluation of the antiproliferative activity in human solid tumor cell lines provided 7-hydroxy-beta-lapachone as lead with enhanced activity over the parent drug beta-lapachone. Cell cycle studies, protein expression experiments, and reactive oxygen species analysis revealed that, similarly to beta-lapachone, ROS formation and DNA damage are critical factors in the cellular toxicity of 7-hydroxy-beta-lapachone. (C) 2012 Elsevier Masson SAS. All rights reserved.
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