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Volumn 20, Issue 12, 2010, Pages 3632-3635

Tricyclic sulfones as orally active γ-secretase inhibitors: Synthesis and structure-activity relationship studies

Author keywords

Secretase; Alzheimer's disease; Sulfone

Indexed keywords

GAMMA SECRETASE; GAMMA SECRETASE INHIBITOR; SULFONAMIDE; SULFONE DERIVATIVE; TRICYCLIC SULFONE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 77954213459     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.04.104     Document Type: Article
Times cited : (27)

References (16)
  • 6
    • 77954213358 scopus 로고    scopus 로고
    • Smith, D. W.; Munoz, B.; Srinivasan, K.; Bregstrom, C. P.; Chaturvedula, P. V.; Deshpande, M. S.; Keavy, D. J.; Lau, W. Y.; Parker, M. F.; Sloan, C. P.; Wallace, O. B.; Wang, H. H. WO 200050391
    • Smith, D. W.; Munoz, B.; Srinivasan, K.; Bregstrom, C. P.; Chaturvedula, P. V.; Deshpande, M. S.; Keavy, D. J.; Lau, W. Y.; Parker, M. F.; Sloan, C. P.; Wallace, O. B.; Wang, H. H. WO 200050391.
  • 13
    • 77954214302 scopus 로고    scopus 로고
    • note
    • 3, 400 MHz) δ 7.80 (m, 4H), 7.08 (m, 1H), 6.42 (m, 1H), 5.16 (d, 1H), 4.22 (d, 1H), 3.71 (s, 3H), 3.02 (d, 1H), 2.60 (d, 1H), 2.45 (m, 1H), 1.97 (m, 2H), 1.75 (m, 1H), 1.58 (m, 1H), 1.07 (m, 1H).
  • 14
    • 0035942322 scopus 로고    scopus 로고
    • Efficacy of γ-secretase inhibitors in intact cells was measured using HEK293 cells expressing human APP with both Swedish and London mutations. The cells were grown in 96-well plate with 100 μL media per well, and were changed to fresh media and incubated with γ-secretase inhibitor for 4 h. Ten microliters of conditioned media was used to measure Aβ40 using ECL technology as described in the following reference. L. Zhang, L. Song, G. Terracina, Y. Liu, B. Pramanik, and E. Parker Biochemistry 40 2001 5049
    • (2001) Biochemistry , vol.40 , pp. 5049
    • Zhang, L.1    Song, L.2    Terracina, G.3    Liu, Y.4    Pramanik, B.5    Parker, E.6
  • 15
    • 77954212903 scopus 로고    scopus 로고
    • note
    • For example, Compound 17b showed 86% inhibition of Aβ40 in plasma and 48% in brain at 10 mg/kg po and compound 15c showed 101% inhibition of Aβ40 in plasma and 71% in brain at 10 mg/kg po.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.