Synthesis and biological activity of new bispyridinium salts of 4,4'-bispyridyl-5,5'-perfluoroalkyl-2,2'-bisoxazoles
Autor: | M. T. Murillo, M. I. Monterde, Y. Martin‐Cantalejo, B. Saez, M. F. Brana |
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Rok vydání: | 2011 |
Předmět: |
Choline kinase
Stereochemistry Pyridines Natural-Products Antineoplastic Agents Chemistry Techniques Synthetic Bisoxazol Antiproliferative Activity Electron Transport Tratamiento médico Inhibitory Concentration 50 Drug Discovery Inhibitory concentration 50 Choline Kinase Humans Pharmacology & Pharmacy Enzyme Inhibitors Oxazoles Cell Proliferation Pharmacology Chemistry Organic Chemistry Choline Kinase Inhibitors Biological activity General Medicine Cáncer Inhibitory Activity Cell culture Bispyridinium Molecular targets Salts Antiproliferative HT29 Cells Human colon |
Zdroj: | European journal of medicinal chemistry. 46(11) |
ISSN: | 1768-3254 |
Popis: | A series of bispyridinium compounds were synthesized by a short sequence of reactions from symmetric diamides. All compounds were tested for their antiproliferative activity against HT-29, a cell line derived from a human colon adenocarcinoma, and their inhibitory activity against choline kinase (ChoK), a novel anticancer molecular target already in clinical trials. Most of the compounds analyzed showed good antiproliferative activities, in the micromolar range, with the identification of promising lead molecules as a new family of potential inhibitors of ChoK. (C) 2011 Elsevier Masson SAS. All rights reserved. 3.346 JCR (2011) Q1, 13/59 Chemistry, medical |
Databáze: | OpenAIRE |
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