Acyl dipeptides as reversible caspase inhibitors. Part 1: initial lead optimization.
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.
Linton
Steven D
SD
Idun Pharmaceuticals, Inc., 9380 Judicial Drive, San Diego, CA 92121, USA. slinton@idun.com
Karanewsky
Donald S
DS
Ternansky
Robert J
RJ
Wu
Joe C
JC
Pham
Brian
B
Kodandapani
Lalitha
L
Smidt
Robert
R
Diaz
Jose-Luis
JL
Fritz
Lawrence C
LC
Tomaselli
Kevin J
KJ
D000215:Acylation; D061945:Caspase Inhibitors; D004151:Dipeptides / Q000138:chemical synthesis* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D007527:Isoenzymes / Q000037:antagonists & inhibitors; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship
D061945:Caspase Inhibitors; D004151:Dipeptides; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D007527:Isoenzymes; D009842:Oligopeptides