Document Detail


Dimers from dechlorinated rebeccamycin: synthesis, interaction with DNA, and antiproliferative activities.
MedLine Citation:
PMID:  12008058     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
In the course of structure-activity relationships on rebeccamycin analogues, two dimers of dechlorinated rebeccamycin were synthesised with the aim to improve the interaction with DNA and in vitro antiproliferative activities. The synthesis of two dimeric compounds obtained by joining two molecules of dechlorinated rebeccamycin via the imide nitrogen is described. Melting temperature and DNase I footprinting studies were performed to investigate their interaction with DNA. Four tumour cell lines, murine L1210 leukaemia, human HT29 colon carcinoma, A549 non-small cell lung carcinoma and K-562 leukaemia, were used to evaluate the cytotoxicity of the drugs. Their effects on the cell cycle of L1210 cells were also investigated.
Authors:
Christelle Marminon; Michaël Facompré; Christian Bailly; John Hickman; Alain Pierré; Bruno Pfeiffer; Pierre Renard; Michelle Prudhomme
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  European journal of medicinal chemistry     Volume:  37     ISSN:  0223-5234     ISO Abbreviation:  Eur J Med Chem     Publication Date:  2002 May 
Date Detail:
Created Date:  2002-05-14     Completed Date:  2003-01-13     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  0420510     Medline TA:  Eur J Med Chem     Country:  France    
Other Details:
Languages:  eng     Pagination:  435-40     Citation Subset:  IM    
Affiliation:
Université Blaise Pascal, Synthèse et Etude de Systèmes à Intérêt Biologique, UMR 6504 du CNRS, F-63177 Aubière, France.
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MeSH Terms
Descriptor/Qualifier:
Aminoglycosides*
Anti-Bacterial Agents / chemical synthesis*,  chemistry,  pharmacology
Carbazoles*
Cell Division / drug effects
Chlorine / chemistry*
DNA / metabolism*
DNA Footprinting
DNA Topoisomerases, Type I / antagonists & inhibitors
Dimerization
Humans
Indoles*
Tumor Cells, Cultured
Chemical
Reg. No./Substance:
0/Aminoglycosides; 0/Anti-Bacterial Agents; 0/Carbazoles; 0/Indoles; 7782-50-5/Chlorine; 9007-49-2/DNA; 93908-02-2/rebeccamycin; EC 5.99.1.2/DNA Topoisomerases, Type I

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


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