5 research outputs found
Lewis Acid-Promoted Reactions of Styrenyl Systems with Benzoquinone Bisimines: New Regioselective Syntheses of Substituted 2-Aryl-2,3-dihydroindoles and 2-Arylindoles
Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization
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
Structure-activity relationships within a series of caspase inhibitors. Part 2: Heterocyclic warheads
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
Structure-activity relationships within a series of caspase inhibitors: effect of leaving group modifications
Various aryloxy methyl ketones of the 1-naphthyloxyacetyl-Val-Asp backbone have been prepared. A systematic study of their structure-activity relationship (SAR) related to caspases 1, 3, 6, and 8 is reported. Highly potent irreversible broad-spectrum caspase inhibitors have been identified. Their efficacy in cellular models of cell death and inflammation are also discussed
Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke
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