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Volumn 21, Issue 11, 2011, Pages 3452-3456

3-Amino-pyrazolo[3,4-d]pyrimidines as p38α kinase inhibitors: Design and development to a highly selective lead

Author keywords

Kinase; Kinase inhibitor; p38

Indexed keywords

3 AMINO PYRAZOLO[3,4 D]PYRIMIDINE; MITOGEN ACTIVATED PROTEIN KINASE P38 INHIBITOR; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 79956123752     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.03.098     Document Type: Article
Times cited : (28)

References (25)
  • 14
    • 79956070010 scopus 로고    scopus 로고
    • Representative experimental procedures for compounds can be found in WO 2007/023110
    • Representative experimental procedures for compounds can be found in WO 2007/023110.
  • 16
    • 84856076831 scopus 로고    scopus 로고
    • 8 compound 23 at 10 μM displaces ligands for the following kinases at the percents indicated: p38α, p38β, JNK1, JNK2, and JNK3 (100%); CSNK1E (88%); GAK (87%); and STK36 (74%). Ambit Kd's were determined for p38α (1.2 nM), p38β (8.7 nM), JNK1 (110 nM), JNK2 (16 nM) and JNK3 (16 nM)
    • 8 compound 23 at 10 μM displaces ligands for the following kinases at the percents indicated: p38α, p38β, JNK1, JNK2, and JNK3 (100%); CSNK1E (88%); GAK (87%); and STK36 (74%). Ambit Kd's were determined for p38α (1.2 nM), p38β (8.7 nM), JNK1 (110 nM), JNK2 (16 nM) and JNK3 (16 nM).
  • 18
    • 79956149738 scopus 로고    scopus 로고
    • note
    • 3S) C, H, N. Specific rotation (MeOH)-34.000 °/g/100 mL.
  • 19
    • 79956131067 scopus 로고    scopus 로고
    • note
    • All animal procedures were approved by the Institutional Animal Care and Use Committee of Roche Palo Alto. Compound was administered (p.o.) to Hanover-Wistar rats 0.5 h prior to challenge with 50 μg/kg LPS (i.e., 0.9% saline). Serum was collected 1.5 h after LPS injection and analyzed for TNF-α levels (ELISA) and drug concentrations.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.