N-Benzylisatin Sulfonamide Analogues as Potent Caspase-3 Inhibitors: Synthesis, in Vitro Activity, and Molecular Modeling Studies

Citations Over TimeTop 23% of 2005 papers

Abstract

A number of isatin sulfonamide analogues were prepared and their potencies for inhibiting caspase-1, -3, -6, -7, and -8 were evaluated in vitro. Several compounds displaying a nanomolar potency for inhibiting the executioner caspases, caspase-3 and caspase-7, were identified. These compounds were also observed to have a low potency for inhibiting the initiator caspases, caspase-1 and caspase-8, and caspase-6. Molecular modeling studies provided further insight into the interaction of this class of compounds with activated caspase-3. The results of the current study revealed a number of non-peptide-based caspase inhibitors that may be useful in assessing the role of inhibiting the executioner caspases in minimizing tissue damage in disease conditions characterized by unregulated apoptosis.

Related Papers

• → Caspase-1 Promiscuity Is Counterbalanced by Rapid Inactivation of Processed Enzyme(2011)85 cited
• → Delineation of the caspase-9 signaling cascade(2007)65 cited
• → Identification of Caspase-6 and Caspase-7 from miiuy croaker and evolution analysis in fish(2018)16 cited
• → Identification of a new caspase homologue: caspase-14(1998)141 cited
• → Caspase cascade of apoptosis induced by satratoxin G in HL-60 cells: possible involvement of caspase-2 in direct activation of caspase-3(2003)