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Volumn 20, Issue 8, 2010, Pages 2560-2563

Amide-based inhibitors of p38α MAP kinase. Part 2: Design, synthesis and SAR of potent N-pyrimidyl amides

Author keywords

Antiinflammatory; Kinase; MAP; p38

Indexed keywords

AMIDE; AMINE; BENZYL DERIVATIVE; CYTOCHROME P450 3A4; FURAN DERIVATIVE; MITOGEN ACTIVATED PROTEIN KINASE 14; MITOGEN ACTIVATED PROTEIN KINASE P38 INHIBITOR; PYRIMIDINE DERIVATIVE;

EID: 77950045753     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.02.090     Document Type: Article
Times cited : (5)

References (27)
  • 19
    • 77950052248 scopus 로고    scopus 로고
    • Luedtke, G. R.; Schinzel, K.; Tan, X.; Tester, R. W.; Nashashibi, I.; Xu, Y.-j.; Dugar, S.; Levy, D. E.; Jung, J. Bioorg. Med. Chem. Lett. doi:10.1016/j.bmcl.2010.02.088.
    • Luedtke, G. R.; Schinzel, K.; Tan, X.; Tester, R. W.; Nashashibi, I.; Xu, Y.-j.; Dugar, S.; Levy, D. E.; Jung, J. Bioorg. Med. Chem. Lett. doi:10.1016/j.bmcl.2010.02.088.
  • 20
    • 77950049768 scopus 로고    scopus 로고
    • note
    • Docking studies were conducted using a high-resolution p38α X-ray structure of p38α (PDB ID: 1ove). The extra-precision mode of Glide, a ligand-receptor docking tool from Schrodinger, LLC, was used to generate a number of poses for analogs 3, 8e, and 8l, which were further filtered by visual inspection.
  • 22
    • 77950049016 scopus 로고    scopus 로고
    • The LPS/TNFα Human Whole Blood Assay was run as described in Mavunkel, B, Dugar, S, Luedtke, G, Tan, X, McEnroe, G. U.S. patent 6,696,443, 2004
    • The LPS/TNFα Human Whole Blood Assay was run as described in Mavunkel, B.; Dugar, S.; Luedtke, G.; Tan, X.; McEnroe, G. U.S. patent 6,696,443, 2004.
  • 26
    • 77950047214 scopus 로고    scopus 로고
    • Tester, R.; Tan, X.; Schinzel, K.; Nashashibi, I.; Luedtke, G. R.; Liang, W.; Jung, J.; Goehring, R. R.; Dugar, S.; Do, S. US 2006/199821, 2006.
    • Tester, R.; Tan, X.; Schinzel, K.; Nashashibi, I.; Luedtke, G. R.; Liang, W.; Jung, J.; Goehring, R. R.; Dugar, S.; Do, S. US 2006/199821, 2006.
  • 27
    • 77950031984 scopus 로고    scopus 로고
    • note
    • 5 Supersomes™, 50 mM 7-benzyloxy-4-(trifluoromethyl)-coumarin, 0.5 M potassium phosphate) was dispensed to columns 1 through 11. The liquid was dispensed in a stream to facilitate mixing. The lid was replaced and incubation continued at 37 °C for 30 min. With a miltichannel pipette, 0.075 mL of STOP solution (80% acetonitrile/20% 0.5 M tris base) was dispensed to all wells. Dispense the liquid in a stream to facilitate mixing. The enzyme/substrate mix (0.1 mL) was dispensed to the wells in column 12 and the plate was scanned with a fluorescent plate scanner (Perkin Elmer LS50B-excitation filter 409 nM, emission filter 530 nM).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.