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Volumn 16, Issue 16, 2006, Pages 4360-4365

The development of novel C-2, C-8, and N-9 trisubstituted purines as inhibitors of TNF-α production

Author keywords

MAP kinase; Mutated p38; p38; Purines; THP 1; THP 1 cell; TNF

Indexed keywords

LIPOPOLYSACCHARIDE; PURINE DERIVATIVE; SYNAPTOPHYSIN; TUMOR NECROSIS FACTOR ALPHA INHIBITOR;

EID: 33745713217     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.05.050     Document Type: Article
Times cited : (14)

References (40)
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    • For recent reviews, see:. Adams J.L., Badger A.M., Kumar S., and Lee J.C. In: King F.D., and Oxford A.W. (Eds). Progress in Medicinal Chemistry Vol. 38 (2001), Elsevier, Amsterdam 1-60
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    • Adams, J.L.1    Badger, A.M.2    Kumar, S.3    Lee, J.C.4
  • 7
    • 0037032817 scopus 로고    scopus 로고
    • For representations of the MAPK signaling cascade, see Refs. 2a,d,e
    • Johnson G.L., and Lapadat R. Science 298 (2002) 1911 For representations of the MAPK signaling cascade, see Refs. 2a,d,e
    • (2002) Science , vol.298 , pp. 1911
    • Johnson, G.L.1    Lapadat, R.2
  • 28
    • 33745732405 scopus 로고
    • 1H NMR) see: The unwanted regioisomer was removed after the second desired displacement (intermediates 2 and 4).
    • 1H NMR) see:. Taylor E.C., and Thompson M.J. J. Org. Chem. 26 (1961) 5224 The unwanted regioisomer was removed after the second desired displacement (intermediates 2 and 4).
    • (1961) J. Org. Chem. , vol.26 , pp. 5224
    • Taylor, E.C.1    Thompson, M.J.2
  • 32
    • 33745718500 scopus 로고    scopus 로고
    • note
    • 15 (Promega Co., Madison, WI).
  • 35
    • 33745704463 scopus 로고    scopus 로고
    • note
    • 19 X-ray data were collected at beamline 17-BM in the facilities of the Industrial Macromolecular Crystallography Association Collaborative Access Team (IMCA-CAT) at the Advanced Photon Source. These facilities are supported by the companies of the Industrial Macromolecular Crystallography Association through a contract with Illinois Institute of Technology (IIT), executed through IIT's Center for Synchrotron Radiation Research and Instrumentation. Use of the Advanced Photon Source was supported by the US Department of Energy, Basic Energy Sciences, Office of Science, under Contract No. W-31-109-Eng-38.
  • 39
    • 33745690250 scopus 로고    scopus 로고
    • Measured as percent loss at 4 h in rat hepatocytes.
  • 40
    • 33745690251 scopus 로고    scopus 로고
    • In vitro metabolism assay procedure: In vitro metabolic stability of analogs in plated rat hepatocytes (Sprague-Dawley) obtained from Cedra Corporation. Metabolic activity was determined in triplicate using a total volume of 0.2 mL containing 0.25 μM NCE incubated in rat hepatocyte and matrigel blank microtiter plates. The plates were maintained at 37 °C throughout the study. Samples were removed from wells at 0, 2, and 4 h, and NCE samples were analyzed by HP-LC/MS/MS with reverse-phase chromatography. To improve analytical efficiency, compounds were grouped together (post-incubation) into a multi-compound assay. Samples from like time-points containing the different compounds were combined and an internal standard (1.1 ng/mL stock) was added. Results for each compound were expressed as the ratio of the compound response area over the internal standard response area. Percent loss was calculated by dividing the 2 and 4 h ratios by the 0 h ratio.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.