“Click” synthesis of small-molecule inhibitors targeting caspases
- 4 February 2008
- journal article
- research article
- Published by Royal Society of Chemistry (RSC) in Organic & Biomolecular Chemistry
- Vol. 6 (5), 844-847
- https://doi.org/10.1039/b718304f
Abstract
A panel of 198 P4-diversified aldehyde (reversible) and vinyl sulfone (irreversible) inhibitors is successfully synthesized via an efficient “click chemistry” platform and directly screened against caspase-3 and -7 for inhibition.This publication has 26 references indexed in Scilit:
- Backbone amide linker (BAL) strategy forNα-9-fluorenylmethoxycarbonyl (Fmoc) solid-phase synthesis of peptide aldehydesJournal of Peptide Science, 2005
- In Situ Selection of Lead Compounds by Click Chemistry: Target-Guided Optimization of Acetylcholinesterase InhibitorsJournal of the American Chemical Society, 2005
- Reducing the Peptidyl Features of Caspase-3 Inhibitors: A Structural AnalysisJournal of Medicinal Chemistry, 2004
- A Potent and Highly Selective Inhibitor of Human α-1,3-Fucosyltransferase via Click ChemistryJournal of the American Chemical Society, 2003
- Discovery of a Potent, Selective Protein Tyrosine Phosphatase 1B Inhibitor Using a Linked-Fragment StrategyJournal of the American Chemical Society, 2003
- Irreversible Inhibitors of Serine, Cysteine, and Threonine ProteasesChemical Reviews, 2002
- Identification of Potent and Selective Small-Molecule Inhibitors of Caspase-3 through the Use of Extended Tethering and Structure-Based Drug DesignJournal of Medicinal Chemistry, 2002
- A Stepwise Huisgen Cycloaddition Process: Copper(I)-Catalyzed Regioselective “Ligation” of Azides and Terminal AlkynesAngewandte Chemie, 2002
- Copper-Catalyzed Enantioselective Henry Reactions of α-Keto Esters: An Easy Entry to Optically Active β-Nitro-α-hydroxy Esters and β-Amino-α-hydroxy EstersThe Journal of Organic Chemistry, 2002
- Cysteine Proteases and Their InhibitorsChemical Reviews, 1997