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Volumn 14, Issue 2, 2004, Pages 351-355

Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: Effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding

Author keywords

[No Author keywords available]

Indexed keywords

POTASSIUM CHANNEL HERG; QUINOLINE DERIVATIVE; VASCULOTROPIN INHIBITOR; VASCULOTROPIN RECEPTOR 2;

EID: 0346729888     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2003.11.007     Document Type: Article
Times cited : (57)

References (30)
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    • (2000) Nat. , vol.407 , pp. 249
    • Carmeliet, P.1    Jain, R.K.2
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    • For reviews, see: (a) Carmeliet P., Jain R.K. Nat. 407:2000;249 (b) Folkman J. Nat. Med. 1:1995;27.
    • (1995) Nat. Med. , vol.1 , pp. 27
    • Folkman, J.1
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    • 0036928020 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.
    • (2002) Expert Opin. Ther. Pat. , vol.12 , pp. 1763
    • Connell, R.D.1
  • 19
    • 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.
    • (2002) Curr. Top. Med. Chem. , vol.2 , pp. 973
    • Boyer, S.J.1
  • 22
    • 0033525530 scopus 로고    scopus 로고
    • 50 value
    • 50 value.
  • 23
    • 85030918771 scopus 로고    scopus 로고
    • 50 value represents the inhibition of VEGF-stimulated mitogenesis as determined in human umbilical vein endothelial cells. Refer to U.S. Patent 6,306,874 for assay details. Values are reported as the average of at least two determinations
    • 50 value represents the inhibition of VEGF-stimulated mitogenesis as determined in human umbilical vein endothelial cells. Refer to U.S. Patent 6,306,874 for assay details. Values are reported as the average of at least two determinations.
  • 26
    • 0035142612 scopus 로고    scopus 로고
    • The hERG IP values were determined through binding competition experiments using membrane preparations from human embryonic kidney cells that constitutively express hERG. For an overview of currently available drug cardiotoxicity assays, see
    • The hERG IP values were determined through binding competition experiments using membrane preparations from human embryonic kidney cells that constitutively express hERG. For an overview of currently available drug cardiotoxicity assays, see Netzer R., Ebneth A., Bischoff U., Pongs O. Drug Discov. Today. 6:2001;78.
    • (2001) Drug Discov. Today , vol.6 , pp. 78
    • Netzer, R.1    Ebneth, A.2    Bischoff, U.3    Pongs, O.4
  • 28
    • 85030917553 scopus 로고    scopus 로고
    • Partition coefficients were determined by HPLC analysis using the octanol/aqueous shake flask method
    • Partition coefficients were determined by HPLC analysis using the octanol/aqueous shake flask method.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.