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Isatin analogues were reported to be selective caspase3/7 inhibitors (see: Lee, D.; Long, S. A.; Adams, J. L.; Chan, G.; Vaidya, K. S.; Francis, T. A.; Kirly, K.; Winkler, J. D.; Sung, C.-M.; Debouck, C.; Richardson, S.; Levy, M. A.; DeWolf, W. E., Jr.; Keller, P. M.; Tomaszek, T.; Head, M. S.; Ryan, M. D.; Haltiwanger, R. C.; Liang, P.-H.; Jan, C. A.; McDevitt, P. J.; Johanson, K. ; Concha, N. O.; Chan, W.; Abdel-Meguid, S. S.; Badger, A. M.; Lark, M. W.; Nadeau, D. P.; Suva, L. J.; Gowen, M.; Nutall, M. E. J. Biol. Chem. 2000, 275, 16007). These compounds have potential drawbacks due to the high reactivity of the ketone carbonyl group.
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more..
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1′ position greatly affected the activity, selectivity and reversibility of casp-1 inhibitors; see:
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Ketone N was prepared according to the literature procedure, see:
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85030912737
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The potency of compounds to inhibit camptothecin induced apoptotic cell death in the neuronal precursor (NT2) cells was determined as described by the testing kit from Roche Molecular Biochemicals, Cat. No. 1,920,685
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The potency of compounds to inhibit camptothecin induced apoptotic cell death in the neuronal precursor (NT2) cells was determined as described by the testing kit from Roche Molecular Biochemicals, Cat. No. 1,920,685.
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22
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85030914440
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Han, Y.10
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Renaud, J.12
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