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Studies on aromatic compounds: inhibition of calpain I by biphenyl derivatives and peptide-biphenyl hybrids

AuthorsMontero, Ana; Alonso Giner, Mercedes; Benito Cano, Esperanza ; Chana López, Antonio ; Mann, Enrique ; Navas, José M.; Herradón García, Bernardo
KeywordsCalpain inhibitor
Peptide-biphenyl hybrids
Aromatic compounds
Issue Date23-Apr-2004
CitationBioorganic & Medicinal Chemistry Letters 14(11): 2753-2757 (2004)
AbstractWith the objective to understand structural features responsible for the biological activity, novel nonelectrophilic biphenyl derivatives and peptide-biphenyl hybrids have been synthesized and evaluated as calpain I inhibitors. The preliminary results indicate that the presence of additional aromatic rings (besides the biphenyl system) makes these compounds potent calpain inhibitors with IC50 values in the nanomolar range.
Description5 pages, 2 figures, 1 table, 2 schemes.-- PMID: 15125927 [PubMed].-- Printed version published Jun 7, 2004.
Taken in part from the Ph. D. thesis of AC (Complutense University, Madrid, 2003) and the projected Ph. D. thesis of AM and MA. Spanish patent ES-P200301125 was filed as of Feb 16, 2006.
Publisher version (URL)http://dx.doi.org/10.1016/j.bmcl.2004.03.071
Appears in Collections:(IQOG) Artículos
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