Bioorganic & Medicinal Chemistry Letters 2002-10-21

Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization.

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

Index: Bioorg. Med. Chem. Lett. 12(20) , 2973-5, (2002)

Full Text: HTML

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.