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Volumn 16, Issue 16, 2006, Pages 4233-4236

Synthesis and evaluation of novel 1-(2-acylhydrazinocarbonyl)-cycloalkyl carboxamides as interleukin-1β converting enzyme (ICE) inhibitors

Author keywords

ICE; Inhibitor; Interleukin 1 converting enzyme; Peptidomimetic scaffold

Indexed keywords

AMIDE; CASPASE 3; CASPASE 8; CYSTEINE PROTEINASE; ENZYME INHIBITOR; INTERLEUKIN 1; INTERLEUKIN 1BETA CONVERTING ENZYME INHIBITOR;

EID: 33745684871     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.05.076     Document Type: Article
Times cited : (7)

References (23)
  • 11
    • 0021149796 scopus 로고
    • Azapeptides have long been used as dipeptide isosteres for enzyme inhibitors, including for example
    • Azapeptides have long been used as dipeptide isosteres for enzyme inhibitors, including for example. Greenlee W.J., Thorsett E.D., Springer J.P., and Patchett A.A. Biochem. Biophys. Res. Commun. 122 (1984) 791
    • (1984) Biochem. Biophys. Res. Commun. , vol.122 , pp. 791
    • Greenlee, W.J.1    Thorsett, E.D.2    Springer, J.P.3    Patchett, A.A.4
  • 17
    • 33745704282 scopus 로고    scopus 로고
    • note
    • 3OD): δ 24.91, 33.67, 34.82, 61.54, 105.05, 124.66, 125.37, 125.83, 126.45, 126.98, 128.19, 130.53, 131.04, 131.85, 133.93, 173.19. MS (ESI): m/e = 426.14 (M+H).
  • 18
    • 33745704281 scopus 로고    scopus 로고
    • Batchelor, M. J.; Bebbington, D.; Bemis, G. W.; Fridman, W. H.; Gillespie, R. J.; Golec, J. M. C.; Gu, Y.; Lauffer, D. J.; Livingston, D. J.; Matharu, S. S.; Mullican, M. D.; Murcko, M. A.; Murdoch, R.; Nyce, P. L.; Robidoux, A. L. C.; Su, M.; Wannamaker, M.; Wilson, K. P.; Zelle, R. E. PCT Intl. Appl. WO 9722619, 1997.
  • 19
    • 33745690070 scopus 로고    scopus 로고
    • note
    • 0 was the initial velocity in the absence of inhibitor.
  • 20
    • 33745704280 scopus 로고    scopus 로고
    • note
    • 6/mL in RPMI 1640 medium from Gibco BRL) was plated in 96-well plates, incubated with or without compounds (administered as solutions in DMSO, such that test concentrations ranged from 1 nM to 10 μM) for 15 min, and then stimulated with LPS (1 μg/mL) for a total of 4 h. Cells were centrifuged and the conditioned media were collected to quantify the release of IL-1β by an ELISA measurement according to the manufacturer's instructions (R&D Systems, catalog number DLB50) or stored at -20 °C for future use.
  • 23
    • 33745704278 scopus 로고    scopus 로고
    • Ellis, C. D.; Oppong, K. A.; Laufersweiler, M. C.; O'Neil, S. V.; Soper, D. L.; Wang, Y.; Wos, J. A.; Fancher, A. N.; Lu, W.; Suchanek, M. K.; Wang, R. L; De, B. 29th National Medicinal Chemistry Symposium, Madison, WI, June 2004, Abstract 110.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.