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Synthesis and biological evaluation of fluoro analogues of antimitotic phenstatin.
MedLine Citation:
PMID:  23618708     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
With the aim of investigating the influence of fluorine, in particular on the A-ring, a new series of fluoro analogues (7a-l) of phenstatin (3) was synthesized and tested for interactions with tubulin polymerization and evaluated for cytotoxicity on an NCI-60 human cancer cell lines panel. We have shown that the replacement of 3,4,5-trimethoxyphenyl A-ring of phenstatin with 2,4,5-trifluoro-3-methoxyphenyl unit, results in the conservation of both antitubulin and cytotoxic effect. Fluoro isocombretastatin 7k was the most effective anticancer agent in the present study and demonstrated the highest antiproliferative potential on leukemia cell lines SR (GI50=15nM) and HL-60(TB) (GI50=23nM) and on melanoma cell line MDA-MB-435 (GI50=19nM).
Authors:
Alina Ghinet; Aurélien Tourteau; Benoît Rigo; Vivien Stocker; Marie Leman; Amaury Farce; Joëlle Dubois; Philippe Gautret
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-4-4
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  -     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2013 Apr 
Date Detail:
Created Date:  2013-4-26     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2013 Elsevier Ltd. All rights reserved.
Affiliation:
Department of Organic Chemistry, 'Al. I. Cuza' University of Iasi, Faculty of Chemistry, Bd., Carol I, nr. 11, 700506 Iasi, Romania; Univ Lille Nord de France, F-59000 Lille, France; UCLille, EA GRIIOT (4481), Laboratoire de Pharmacochimie, HEI, 13 Rue de Toul, F-59046 Lille, France.
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