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Volumn 19, Issue 11, 2009, Pages 3136-3140

Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase

Author keywords

IGF 1R; IGF IR; Kinase inhibitor; Pyrrolopyridine

Indexed keywords

3,4 DISUBSTITUTED 1H PYRROLO[2,3 BETA]PYRIDINE; PROTEIN TYROSINE KINASE INHIBITOR; PYRIDINE DERIVATIVE; PYRROLOPYRIDINE INHIBITOR; SOMATOMEDIN C RECEPTOR; UNCLASSIFIED DRUG;

EID: 65149102076     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.12.110     Document Type: Article
Times cited : (25)

References (21)
  • 2
    • 38849088141 scopus 로고    scopus 로고
    • (and references therein)
    • Ryan P.D., and Goss P.E. Oncologist 13 (2008) 16 (and references therein)
    • (2008) Oncologist , vol.13 , pp. 16
    • Ryan, P.D.1    Goss, P.E.2
  • 12
    • 65149106189 scopus 로고    scopus 로고
    • note
    • 2, 0.1 mg/ml BSA, at room temperature. Compounds, titrated in DMSO, were evaluated at eleven concentrations ranging from 50 μM to 0.2 nM. Reactions were incubated for 1 h at room temperature and were stopped by a 5-μl addition of EDTA (to 33 mM). A further addition of 5 μl detection reagents (for final 7 nM Streptavidin-APC (Perkin-Elmer #CR130-150), 1 nM Europium-labeled anti-phosphotyrosine monoclonal antibody (Perkin-Elmer #AD0067), added in reaction buffer (without DTT), was required for signal generation. After 30 minutes, signal was read on Perkin-Elmer Viewlux microplate imager or Wallac Victor fluorometer as subtracted from all samples for background).
  • 14
    • 65149083641 scopus 로고    scopus 로고
    • Arnold, W. D.; Bounaud, P.; Gosberg, A.; Li, Z.; McDonald, I.; Steensma, R. W.; Wilson, M. E. WO2006015123-A1, 2006.
    • Arnold, W. D.; Bounaud, P.; Gosberg, A.; Li, Z.; McDonald, I.; Steensma, R. W.; Wilson, M. E. WO2006015123-A1, 2006.
  • 15
  • 16
    • 42949149240 scopus 로고    scopus 로고
    • For a recent discussion of crystal structures of 1H-pyrrolo[2,3-b]pyridines bound to protein kinases, see:
    • For a recent discussion of crystal structures of 1H-pyrrolo[2,3-b]pyridines bound to protein kinases, see:. Tsai J., et al. Proc. Natl. Acad. Sci. U.S.A. 105 (2008) 3041
    • (2008) Proc. Natl. Acad. Sci. U.S.A. , vol.105 , pp. 3041
    • Tsai, J.1
  • 17
    • 65149100255 scopus 로고    scopus 로고
    • note
    • 50) was determined by 4 parameter fit of data using XLfit (value of no cell control was subtracted from all samples for background).
  • 18
    • 65149093269 scopus 로고    scopus 로고
    • note
    • The cellular potencies of 19 and 21, reported in Table 1, were not determined.
  • 19
    • 0028582185 scopus 로고    scopus 로고
    • note
    • factor of 20% at 2.6 Å using REFMAC. Crystallographic data for the structure in Figure 1 have been deposited at PDB:3ETA.
  • 20
    • 5044236233 scopus 로고    scopus 로고
    • For kinase ATP binding pocket nomenclature, see:
    • For kinase ATP binding pocket nomenclature, see:. Vulpetti A., and Bosotti R. Il Farmaco 59 (2004) 759
    • (2004) Il Farmaco , vol.59 , pp. 759
    • Vulpetti, A.1    Bosotti, R.2
  • 21
    • 65149106298 scopus 로고    scopus 로고
    • note
    • Compound 23 inhibited cellular proliferation in a COLO205 cell line with EC50 at 274 nM (average of 4 measurements).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.