Document Detail


Synthesis and antitumor activity of 2,5-bis(3'-indolyl)-furans and 3,5-bis(3'-indolyl)-isoxazoles, nortopsentin analogues.
MedLine Citation:
PMID:  20472437     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A series of novel 2,5-bis(3'-indolyl)furans and 3,5-bis(3'-indolyl)isoxazoles were synthesized as antitumor agents. The antiproliferative activity was evaluated in vitro toward diverse human tumor cell lines. Initially 5 isoxazoles and 3 furan derivatives were tested against a panel of 10 human tumor cell lines and the most active derivatives 3c and 4a were selected to be evaluated in an extended panel of 29 cell lines. By exhibiting mean IC(50) values of 17.4 microg/mL (3a) and 20.5 microg/mL (4c), in particular 4c showed a high level of tumor selectivity toward the 29 cell lines.
Authors:
Patrizia Diana; Anna Carbone; Paola Barraja; Gerhard Kelter; Heinz-Herbert Fiebig; Girolamo Cirrincione
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-04-28
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  18     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2010 Jun 
Date Detail:
Created Date:  2010-06-23     Completed Date:  2010-10-14     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  4524-9     Citation Subset:  IM    
Copyright Information:
Copyright 2010 Elsevier Ltd. All rights reserved.
Affiliation:
Dipartimento Farmacochimico, Tossicologico e Biologico, Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy.
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MeSH Terms
Descriptor/Qualifier:
Antineoplastic Agents / chemical synthesis*,  chemistry,  therapeutic use
Cell Line, Tumor
Drug Screening Assays, Antitumor
Furans / chemical synthesis,  chemistry*,  therapeutic use
Humans
Indoles / chemical synthesis,  chemistry*,  therapeutic use
Isoxazoles / chemical synthesis,  chemistry*,  therapeutic use
Neoplasms / drug therapy
Chemical
Reg. No./Substance:
0/3-3'-furan-2,5-diylbis(1-methyl-1H-indole); 0/3-3'-isoxazole-3,5-diylbis(5-methoxy-1-methyl-1H-indole); 0/Antineoplastic Agents; 0/Furans; 0/Indoles; 0/Isoxazoles

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