Document Detail


Synthesis and biological activities of aminopyrimidyl-indoles structurally related to meridianins.
MedLine Citation:
PMID:  19477650     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The synthesis of new meridianin derivatives substituted at the C-5 position of the 2-aminopyrimidine ring by various aryl groups and substituted or not by a methyl group on the indole nitrogen is described. These compounds were tested for their kinase inhibitory potencies toward five kinases (CDK5/p25, CK1delta/epsilon, GSK-3alpha/beta, Dyrk1A and Erk2) as well as their in vitro antiproliferative activities toward a human fibroblast primary culture and two human solid cancer cell lines (MCF-7 and PA 1).
Authors:
Rufine Akue-Gedu; Eric Debiton; Yoan Ferandin; Laurent Meijer; Michelle Prudhomme; Fabrice Anizon; Pascale Moreau
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-05-12
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  17     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2009 Jul 
Date Detail:
Created Date:  2009-06-12     Completed Date:  2009-09-09     Revised Date:  2009-11-19    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  4420-4     Citation Subset:  IM    
Affiliation:
Clermont Université, Université Blaise Pascal, SEESIB, Aubière, France.
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MeSH Terms
Descriptor/Qualifier:
Animals
Cell Line, Tumor
Cell Proliferation / drug effects*
Cells, Cultured
Fibroblasts / cytology
Humans
Indole Alkaloids / chemical synthesis*,  chemistry,  pharmacology*
Protein Kinase Inhibitors / chemical synthesis*,  chemistry,  pharmacology*
Protein Kinases / metabolism*
Rats
Structure-Activity Relationship
Swine
Chemical
Reg. No./Substance:
0/Indole Alkaloids; 0/Protein Kinase Inhibitors; EC 2.7.-/Protein Kinases

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


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