Document Detail


β-Lapachone analogs with enhanced antiproliferative activity.
MedLine Citation:
PMID:  22560628     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
In this study, we describe the synthesis of a series of α- and β-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-β-lapachone as lead with enhanced activity over the parent drug β-lapachone. Cell cycle studies, protein expression experiments, and reactive oxygen species analysis revealed that, similarly to β-lapachone, ROS formation and DNA damage are critical factors in the cellular toxicity of 7-hydroxy-β-lapachone.
Authors:
Carla Ríos-Luci; Evelyn L Bonifazi; Leticia G León; Juan C Montero; Gerardo Burton; Atanasio Pandiella; Rosana I Misico; José M Padrón
Related Documents :
20069368 - Microfluidic platforms for studies of angiogenesis, cell migration, and cell-cell inter...
22593438 - Effect of mir-34b overexpression on the radiosensitivity of non-small cell lung cancer ...
19232058 - Biochemical evidence of the interactions of membrane type-1 matrix metalloproteinase (m...
7197278 - Specification of cell morphology by endogenous determinants.
23744888 - Adult renal mesenchymal stem cell-like cells contribute to juxtaglomerular cell recruit...
22170698 - Restoration of c/ebpα in dedifferentiated liposarcoma induces g2/m cell cycle arrest a...
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-4-19
Journal Detail:
Title:  European journal of medicinal chemistry     Volume:  -     ISSN:  1768-3254     ISO Abbreviation:  -     Publication Date:  2012 Apr 
Date Detail:
Created Date:  2012-5-7     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0420510     Medline TA:  Eur J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2012 Elsevier Masson SAS. All rights reserved.
Affiliation:
BioLab, Instituto Universitario de Bio-Orgánica "Antonio González", Universidad de La Laguna, C/Astrofísico Francisco Sánchez 2, 38206 La Laguna, Spain.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


Previous Document:  2-Anilino-4-(benzimidazol-2-yl)pyrimidines - A multikinase inhibitor scaffold with antiproliferative...
Next Document:  Synthesis, anti-Candida activity, and cytotoxicity of new (4-(4-iodophenyl)thiazol-2-yl)hydrazine de...