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Volumn 17, Issue 13, 2007, Pages 3550-3557

Novel inhibitors of VEGF receptors-1 and -2 based on azole-5-carboxamide templates

Author keywords

1 (2 (Pyridin 4 yl)ethyl) 1H azole 5 carboxamides; Angiogenesis; Dual kinase inhibitors; Receptor tyrosine kinase; Vascular endothelial growth factor receptor 2; VEGFR 1; VEGFR 2

Indexed keywords

1 [2 (PYRIDIN 4 YL)ETHYL] 1H AZOLE 5 CARBOXAMIDE; ADENOSINE TRIPHOSPHATE DERIVATIVE; AMIDE; CARBOXYLIC ACID DERIVATIVE; N (3,3 DIMETHYL 6 INDOLINYL) 2 (4 PYRIDINYLMETHYLAMINO)NICOTINAMIDE; PHTHALAZINE DERIVATIVE; PYRROLE; UNCLASSIFIED DRUG; VANDETANIB; VASCULOTROPIN INHIBITOR; VASCULOTROPIN RECEPTOR 1; VASCULOTROPIN RECEPTOR 2; VATALANIB;

EID: 34250162117     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.04.042     Document Type: Article
Times cited : (7)

References (33)
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    • ™ (Pegaptanib sodium, Eyetech Pharmaceuticals, New York, NY and Pfizer) has recently been approved to treat neovascular age-related macular degeneration; see
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    • 34250208221 scopus 로고    scopus 로고
    • note
    • 6; δ, ppm): 10.5, 13.2, 33.9, 58.5, 115.2, 122.7, 123.0, 128.9, 130.5, 133.4, 144.7, 145.5, 150.1, 162.4; ESI MS (M+1): 356, (M-1): 354; HRMS, exact mass calcd. ...
  • 28
    • 34250190767 scopus 로고    scopus 로고
    • note
    • 2, and 2 mM DTT, 1 mg/ml BSA) containing 0.5 mmol pGAT-biotin and 3-4 ng KDR enzyme was added to each well. After 5-10-min preincubation, the kinase reaction was initiated by the addition of 10 μl of 10 μM ATP in the reaction buffer, after which the plate was incubated at room temperature for 45 min. The reaction was stopped by addition of 50 μl of KF buffer (50 mM Hepes, pH 7.5, 0.5 M KF, and 1 mg/ml BSA) containing 100 mM EDTA and 0.36 μg/ml PY20K (Eu-cryptate labeled anti-phosphotyrosine antibody, CIS bio international) was added and after an additional 2 h incubation at RT, the plate was analyzed in a RUBYstar HTRF Reader.
  • 29
    • 34250190030 scopus 로고    scopus 로고
    • note
    • 50 represents the concentration of compound that caused 50% reduction in absorbance at 562 nm relative to untreated cells using sulfurhodamine B assay. Values were means of three independent determinations (SD < 10%).
  • 32
  • 33
    • 34250189329 scopus 로고    scopus 로고
    • note
    • 4, absorbance was measured at 450 nm.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.