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Steven D Linton,
Teresa Aja,
Peter R Allegrini,
Thomas L Deckwerth,
Jose-Luis Diaz,
Bastian Hengerer,
Julia Herrmann,
Kathy G Jahangiri,
Joerg Kallen,
Donald S Karanewsky, [......],
Giorgio Rovelli,
Andre Sauter,
Robert O Sayers,
Albert Schmitz, Robert Smidt,
Robert J Ternansky,
Kevin J Tomaselli,
Brett R Ullman,
Christoph Wiessner,
Joe C Wu
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ABSTRACT: Structural modifications were made to a previously described acyl dipeptide caspase inhibitor, leading to the oxamyl dipeptide series. Subsequent SAR studies directed toward the warhead, P2, and P4 regions of this novel peptidomimetic are described herein.
Bioorganic & Medicinal Chemistry Letters 06/2004; 14(10):2685-91. · 2.55 Impact Factor
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[show abstract]
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ABSTRACT: Parallel synthesis was used to explore the SAR of a peptidomimetic caspase inhibitor. The most potent compound had nanomolar activity against caspases 1, 3, 6, 7, and 8.
Bioorganic & Medicinal Chemistry Letters 11/2002; 12(20):2969-71. · 2.55 Impact Factor
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Steven D Linton,
Donald S Karanewsky,
Robert J Ternansky,
Ning Chen,
Xian Guo,
Kathy G Jahangiri,
Vincent J Kalish,
Steven P Meduna,
Edward D Robinson,
Brett R Ullman,
Joe C Wu,
Brian Pham,
Lalitha Kodandapani, Robert Smidt,
Jose-Luis Diaz,
Lawrence C Fritz,
U von Krosigk,
Silvio Roggo,
Albert Schmitz,
Kevin J Tomaselli
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ABSTRACT: A new structural class of broad spectrum caspase inhibitors was optimized for its activity against caspases 1, 3, 6, 7, and 8. The most potent compound had low nanomolar broad spectrum activity, in particular, single digit nanomolar inhibitory activity against caspase 8.
Bioorganic & Medicinal Chemistry Letters 11/2002; 12(20):2973-5. · 2.55 Impact Factor
