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Volumn 15, Issue 5, 2005, Pages 1429-1433

Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors

Author keywords

Angiogenesis; Kinase receptor; SAR; VEGFR 2

Indexed keywords

4 (3 HYDROXY 4 METHYLPHENYLAMINO)PYRROLO[2,1 F][1,2,4]TRIAZINE; PHENOL DERIVATIVE; PHOSPHOTRANSFERASE INHIBITOR; TRIAZINE DERIVATIVE; UNCLASSIFIED DRUG; VASCULOTROPIN INHIBITOR; VASCULOTROPIN RECEPTOR 2;

EID: 13944258781     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.12.079     Document Type: Article
Times cited : (46)

References (16)
  • 9
    • 85030814835 scopus 로고    scopus 로고
    • note
    • 2.5 μM ATP concentration was used in the enzyme assay
  • 11
    • 0016152978 scopus 로고
    • An alternate synthesis of pyrroles 2 could be accomplished using the published route: M. Suzuki, M. Miyoshi, and K. Matsumoto J. Org. Chem. 39 1974 1980
    • (1974) J. Org. Chem. , vol.39 , pp. 1980
    • Suzuki, M.1    Miyoshi, M.2    Matsumoto, K.3
  • 13
    • 85030814410 scopus 로고    scopus 로고
    • note
    • The rate of glucuronidation was determined under the following conditions: substrate concentration, 20 μM; protein concentration, 2 mg/mL; UDPGA, 5 mM; pH 7.5 Tris buffer, 100 mM; magnesium chloride, 10 mM; alamethicine (in ethanol), 2.5 μg/mL. Incubations were performed at 37°C and were initiated by the addition of UDPGA. 200 μL aliquots were taken at times 0, 10, and 20 min and the reaction terminated by the addition of equal volume of acetonitrile. Following vortexing and centrifugation, 20 μL aliquot was analyzed by HPLC-UV. The percentage of compound remaining at each time point was calculated and compared to the values at zero time point. The rate of metabolism was calculated by determining the nanomoles of compound that disappeared and dividing it by the time of incubation and the milligram of protein
  • 14
    • 85030808658 scopus 로고    scopus 로고
    • note
    • 3OD, 300 MHz) of compound 27: δ 7.80 (s, 1H), 7.55 (s, 1H), 7.01 (d, 1H, J = 8 Hz), 6.77 (s, 1H), 6.64 (d, 1H, J = 8 Hz), 3.60-3.47 (m, 3H), 3.29-3.26 (m, 2H), 3.12-3.10 (m, 2H), 3.08-2.89 (m, 2H), 2.04 (s, 3H), 1.99-1.95 (m, 2H), 1.891.82 (m, 3H), 1.32 (d, 6H, J = 7 Hz)


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.