Nicotinyl aspartyl ketones as inhibitors of caspase-3

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 13, 2003, Pages 2137-2140

  Isabel, Elise ^a   Black, W Cameron ^a   Bayly, Christopher I ^a   Grimm, Erich L ^a   Janes, Marc K ^a   McKay, Daniel J ^a   Nicholson, Donald W ^a   Rasper, Dita M ^a   Renaud, Johanne ^a   Roy, Sophie ^a   Tam, John ^a   Thornberry, Nancy A ^b   Vaillancourt, John P ^a   Xanthoudakis, Steven ^a   Zamboni, Robert ^a  

^a MERCK FROSST CENTRE FOR THERAPEUTIC RESEARCH   (Canada)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALDEHYDE DERIVATIVE; AMIDE; ASPARTIC ACID DERIVATIVE; CASPASE 3; CASPASE 3 INHIBITOR; KETONE DERIVATIVE; SULFONAMIDE;

APOPTOSIS; ARTICLE; CONTROLLED STUDY; DEGENERATIVE DISEASE; DRUG POTENTIATION; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; HUMAN CELL; SOLID PHASE EXTRACTION;

EID: 12444344281     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00390-1     Document Type: Article

References (11)

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2. Nicholson D.W. Nature. 407:2000;810. and references therein.
3. Grimm, E. L. Unpublished results.
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7. Kharasch N., Bruice T.C. J. Am. Chem. Soc. 73:1951;3240.
8. 1H NMR.
9. Roy S., Bayly C.I., Gareau Y., Houtzager V.M., Kargan S., Keen S.L., Rowland K., Seiden I.M., Thornberry N.A., Nicholson D.W. Proc. Natl. Acad. Sci. U.S.A. 98:2001;6132.
10. Tawa P., Tam J., Cassady R., Nicholson D.W., Xanthoudakis S. Cell Death Diff. 8:2001;30.
11. NT2 cells were plated in 96-well plates. The following day, camptothecin 5 μg/mL and±different concentrations of the inhibitors were added for 5 h. Cells were then harvested, lysed and analyzed by cell death ELISA following manufacturer kit's instructions (Roche Molecular Biochemicals) measuring DNA fragmentation.