메뉴 건너뛰기




Volumn 21, Issue 22, 2011, Pages 6842-6851

Non-steroidal dissociated glucocorticoid agonists: Indoles as A-ring mimetics and function-regulating pharmacophores

Author keywords

Dissociated activity; Function regulating pharmacophore; Non steroidal glucocorticoid agonist

Indexed keywords

AROMATASE; DEXAMETHASONE; FATTY ACID; GLUCOCORTICOID RECEPTOR; HORMONE RECEPTOR STIMULATING AGENT; INDOLE DERIVATIVE; INSULIN; INTERLEUKIN 6; LIPOPOLYSACCHARIDE; NONSTEROIDAL GLUCOCORTICOID RECEPTOR AGONIST; PREDNISOLONE; TRIACYLGLYCEROL; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG;

EID: 80054719120     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.09.018     Document Type: Article
Times cited : (16)

References (61)
  • 36
    • 80054764129 scopus 로고    scopus 로고
    • In addition to our discovery of indole as A-ring mimetic, research at Boehringer Ingelheim identified quinol-4-ones and azaindoles as attractive A-ring replacements. These are exemplified by the compounds 3 and 4, respectively. These discoveries were published in the recent articles. See Ref. 45,46
    • In addition to our discovery of indole as A-ring mimetic, research at Boehringer Ingelheim identified quinol-4-ones and azaindoles as attractive A-ring replacements. These are exemplified by the compounds 3 and 4, respectively. These discoveries were published in the recent articles. See Ref. 45,46.
  • 37
    • 84857504005 scopus 로고    scopus 로고
    • Glide, version 5.0, Schrödinger, LLC, New York, NY, 2008
    • Glide, version 5.0, Schrödinger, LLC, New York, NY, 2008.
  • 38
    • 84857502859 scopus 로고    scopus 로고
    • 39
    • 39
  • 39
    • 80054768931 scopus 로고    scopus 로고
    • Molecular Operating Environment (MOE), 2010.10; Chemical Computing Group Inc., 1010 Sherbrooke St. West, Suite #910, Montreal, QC, Canada, H3A 2R7, 2010
    • Molecular Operating Environment (MOE), 2010.10; Chemical Computing Group Inc., 1010 Sherbrooke St. West, Suite #910, Montreal, QC, Canada, H3A 2R7, 2010.
  • 49
    • 84857504813 scopus 로고    scopus 로고
    • The fibroblast-IL-6 assay measured the ability of test compounds to inhibit the elaboration of IL-6 by human foreskin fibroblasts (ATCC # CRL-2429) following stimulation by IL-1 (1 ng/mL) in vitro. After incubation at 37 °C for 18-24 h, IL-6 concentration in the tissue culture media was measured using standard electrochemiluminescence, DELFIA, or ELISA methods. In this assay, IL-6 inhibition is a measure of glucocorticoid receptor response to agonist, and dexamethasone was assigned 100% efficacy
    • The fibroblast-IL-6 assay measured the ability of test compounds to inhibit the elaboration of IL-6 by human foreskin fibroblasts (ATCC # CRL-2429) following stimulation by IL-1 (1 ng/mL) in vitro. After incubation at 37 °C for 18-24 h, IL-6 concentration in the tissue culture media was measured using standard electrochemiluminescence, DELFIA, or ELISA methods. In this assay, IL-6 inhibition is a measure of glucocorticoid receptor response to agonist, and dexamethasone was assigned 100% efficacy.
  • 51
    • 84857505423 scopus 로고    scopus 로고
    • 50 value of 1.8 nM
    • 50 value of 1.8 nM.
  • 52
    • 84857504004 scopus 로고    scopus 로고
    • 2 and luminescent signal was detected in lysed cells using Steady-Glo® luciferase reagents (Promega #E2520). Dexamethasone (1 μM) was assigned 100% induction of luminescent signal in this assay
    • 2 and luminescent signal was detected in lysed cells using Steady-Glo® luciferase reagents (Promega #E2520). Dexamethasone (1 μM) was assigned 100% induction of luminescent signal in this assay.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.