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Volumn 13, Issue 18, 2003, Pages 2973-2976

Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors

Author keywords

[No Author keywords available]

Indexed keywords

3 (5 THIEN 3 YLPYRIDIN 3 YL) 1H INDOLE; ENZYME INHIBITOR; INDOLE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 12444275599     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00627-9     Document Type: Article
Times cited : (12)

References (30)
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    • For reviews, see: (a) Carmeliet P., Jain R.K. Nature. 407:2000;249 (b) Folkman J. Nat. Med. 1:1995;27.
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    • For recent reviews, see: (a) Connell R.D. Expert Opin. Ther. Pat. 12:2002;1763 (b) Boyer S.J. Curr. Top. Med. Chem. 2:2002;973 (c) Bilodeau M.T., Fraley M.E., Hartman G.D. Expert Opin. Investig. Drugs. 11:2002;737.
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    • Connell, R.D.1
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    • 0036718947 scopus 로고    scopus 로고
    • For recent reviews, see: (a) Connell R.D. Expert Opin. Ther. Pat. 12:2002;1763 (b) Boyer S.J. Curr. Top. Med. Chem. 2:2002;973 (c) Bilodeau M.T., Fraley M.E., Hartman G.D. Expert Opin. Investig. Drugs. 11:2002;737.
    • (2002) Curr. Top. Med. Chem. , vol.2 , pp. 973
    • Boyer, S.J.1
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    • note
    • 50 value.
  • 20
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    • note
    • 50 value represents the inhibition of VEGF-stimulated mitogenesis as determined in human umbilical vein endothelial cells. Refer to US Patent 6,265,403 for assay details. Values are reported as the average of three determinations for compounds 1 and 3d, and single determinations for 3a, 3e, 3f, and 3h.
  • 21
    • 85031071152 scopus 로고    scopus 로고
    • note
    • Partition coefficients were determined by HPLC analysis in octanol/water.
  • 22
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    • note
    • 1H NMR and mass spectroscopy.
  • 23
    • 4444268000 scopus 로고
    • Compounds 2a-f were prepared by the following sequence; for related chemistry; see
    • Compounds 2a-f were prepared by the following sequence; for related chemistry; see: Lipshutz B.H., Hungate R.W., McCarthy K.E. J. Am. Chem. Soc. 105:1983;7703.
    • (1983) J. Am. Chem. Soc. , vol.105 , pp. 7703
    • Lipshutz, B.H.1    Hungate, R.W.2    McCarthy, K.E.3
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    • 0033026444 scopus 로고    scopus 로고
    • For a description of the ATP binding region of protein tyrosine kinases, see:
    • For a description of the ATP binding region of protein tyrosine kinases, see: Traxler P., Furet P. Pharmacol. Ther. 82:1999;195.
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    • note
    • Additional examples as well as experimental details of the synthetic methods employed in this work can be found in US Patent 6,265,403.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.