title: Studies on aromatic compounds: inhibition of calpain I by biphenyl derivatives and peptide-biphenyl hybrids.
abstract: With 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.
authors.affiliation: Instituto de Química Orgánica General, CSIC, Juan de la Cierva 3, 28006 Madrid, Spain.
authors.forename: Ana
authors.initials: A
authors.lastname: Montero
authors.forename: Mercedes
authors.initials: M
authors.lastname: Alonso
authors.forename: Esperanza
authors.initials: E
authors.lastname: Benito
authors.forename: Antonio
authors.initials: A
authors.lastname: Chana
authors.forename: Enrique
authors.initials: E
authors.lastname: Mann
authors.forename: José M
authors.initials: JM
authors.lastname: Navas
authors.forename: Bernardo
authors.initials: B
authors.lastname: Herradón
mesh_terms: D001713:Biphenyl Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D002154:Calpain / Q000037:antagonists & inhibitors*; D006801:Humans; D020128:Inhibitory Concentration 50; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D001713:Biphenyl Compounds; D009842:Oligopeptides; D011480:Protease Inhibitors; D002154:Calpain