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

Bioorg Med Chem Lett

Instituto de Química Orgánica General, CSIC, Juan de la Cierva 3, 28006 Madrid, Spain.

Published: June 2004

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.

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http://dx.doi.org/10.1016/j.bmcl.2004.03.071DOI Listing

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