Document Detail

A new family of quinoline and quinoxaline analogues of combretastatins.
MedLine Citation:
PMID:  15203159     Owner:  NLM     Status:  MEDLINE    
The 3-hydroxy-4-methoxyphenyl ring of combretastatin A-4 can be replaced by a 2-naphthyl moiety without significant loss of cytotoxicity and inhibition of tubulin polymerization potency. In this paper we show that the 6- or 7-quinolyl systems can in turn replace both cyclic moieties, keeping in the first case most of the potency as cytotoxic agent and in the second case as inhibitor of tubulin polymerization, related to the activities displayed by model compounds.
Concepción Pérez-Melero; Ana B S Maya; Benedicto del Rey; Rafael Peláez; Esther Caballero; Manuel Medarde
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  14     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2004 Jul 
Date Detail:
Created Date:  2004-06-18     Completed Date:  2005-02-07     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  3771-4     Citation Subset:  IM    
Laboratorio de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Salamanca, Campus Miguel de Unamuno, 37007 Salamanca, Spain.
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MeSH Terms
Antineoplastic Agents / chemical synthesis*,  pharmacology
Biopolymers / chemistry
Cell Line, Tumor
Inhibitory Concentration 50
Naphthalenes / chemistry
Quinolines / chemistry*
Quinoxalines / chemistry*
Stilbenes / chemical synthesis*,  pharmacology
Structure-Activity Relationship
Tubulin / chemistry
Tubulin Modulators*
Reg. No./Substance:
0/Antineoplastic Agents; 0/Biopolymers; 0/Ligands; 0/Naphthalenes; 0/Quinolines; 0/Quinoxalines; 0/Stilbenes; 0/Tubulin; 0/Tubulin Modulators; 117048-59-6/combretastatin A-4; 91-22-5/quinoline

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