Ullman Brett R, Aja Teresa, Chen Ning, Diaz Jose-Luis, Gu Xin, Herrmann Julia, Kalish Vincent J, Karanewsky Donald S, Kodandapani Lalitha, Krebs Joseph J, Linton Steven D, Meduna Steven P, Nalley Kip, Robinson Edward D, Roggo Silvio P, Sayers Robert O, Schmitz Albert, Ternansky Robert J, Tomaselli Kevin J, Wu Joe C
Idun Pharmaceuticals Inc., 9380 Judicial Drive, San Diego, CA 92121, USA.
Bioorg Med Chem Lett. 2005 Aug 1;15(15):3632-6. doi: 10.1016/j.bmcl.2005.05.036.
Various heterocyclic hetero-methyl ketones of the 1-naphthyloxyacetyl-Val-Asp backbone have been prepared. A study of their structure-activity relationship (SAR) related to caspase-1, -3, -6, and -8 is reported. Their efficacy in a cellular model of cell death is also discussed. Potent broad-spectrum caspase inhibitors have been identified.