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Structure-activity relationships within a series of caspase inhibitors. Part 2: Heterocyclic warheads.

作者信息

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

机构信息

Idun Pharmaceuticals Inc., 9380 Judicial Drive, San Diego, CA 92121, USA.

出版信息

Bioorg Med Chem Lett. 2005 Aug 1;15(15):3632-6. doi: 10.1016/j.bmcl.2005.05.036.

Abstract

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.

摘要

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