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Volumn 21, Issue 6, 2011, Pages 1626-1629

Isatin 1,2,3-triazoles as potent inhibitors against caspase-3

Author keywords

1,2,3 Triazole; Caspase 3; Inhibitors; Isatin

Indexed keywords

1 [(1 BENZYL 1H 1,2,3 TRIAZOL 5 YL)METHYL] 5 [[2 (METHOXYMETHYL)PYRROLIDIN 1 YL]SULFONYL]INDOLINE 2,3 DIONE; 1 [[1 (2,3 DIHYDRO BENZO[B][1,4]DIOXIN 6 YL) 1H 1,2,3 TRIAZOL 4 YL]METHYL] 5 [[2 (METHOXYMETHYL)PYRROLIDIN 1 YL]SULFONYL]INDOLINE 2,3 DIONE; CASPASE 3; CASPASE 3 INHIBITOR; ISATIN 1,2,3 TRIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 79952362107     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.01.110     Document Type: Article
Times cited : (51)

References (38)
  • 32
    • 79952364551 scopus 로고    scopus 로고
    • + HEPES (pH 7.5), 50 mM KCl, 0.1% CHAPS, 5 mM β-mercaptoethanol, 1 mM EDTA, 10% sucrose and 10 μM Ac-DEVD-AFC. The final concentration of caspase-3 was 0.25 nM (calculated as heterodimer), and the final concentration of DMSO was 5%. Compounds tested were diluted in DMSO prior to the assay
    • + HEPES (pH 7.5), 50 mM KCl, 0.1% CHAPS, 5 mM β-mercaptoethanol, 1 mM EDTA, 10% sucrose and 10 μM Ac-DEVD-AFC. The final concentration of caspase-3 was 0.25 nM (calculated as heterodimer), and the final concentration of DMSO was 5%. Compounds tested were diluted in DMSO prior to the assay.
  • 33
    • 79952361559 scopus 로고    scopus 로고
    • The inhibition kinetics for compounds 7f and 8g against caspase-3 were determined using buffer conditions described above. The concentration of Ac-DEVD-AFC was varied from 6.25 to 100 μM, and the concentration of the inhibitor was varied from 0 to 120 nM and from 0 to 60 nM for compounds 7f and 8g, respectively. The maximum slope of the curve of AFC fluorescence was used as the initial rate
    • The inhibition kinetics for compounds 7f and 8g against caspase-3 were determined using buffer conditions described above. The concentration of Ac-DEVD-AFC was varied from 6.25 to 100 μM, and the concentration of the inhibitor was varied from 0 to 120 nM and from 0 to 60 nM for compounds 7f and 8g, respectively. The maximum slope of the curve of AFC fluorescence was used as the initial rate.
  • 34
    • 79952363107 scopus 로고    scopus 로고
    • i). We are grateful to an anonymous referee for helpful suggestions on how to perform these calculations
    • i). We are grateful to an anonymous referee for helpful suggestions on how to perform these calculations.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.