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pubmed-article:16302804pubmed:abstractTextA 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.lld:pubmed
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pubmed-article:16302804pubmed:dateRevised2007-11-14lld:pubmed
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pubmed-article:16302804pubmed:articleTitleN-benzylisatin sulfonamide analogues as potent caspase-3 inhibitors: synthesis, in vitro activity, and molecular modeling studies.lld:pubmed
pubmed-article:16302804pubmed:affiliationDivision of Radiological Sciences, Washington University School of Medicine, 510 South Kingshighway Boulevard, St. Louis, Missouri 63110, USA.lld:pubmed
pubmed-article:16302804pubmed:publicationTypeJournal Articlelld:pubmed
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