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Volumn 17, Issue 21, 2007, Pages 5978-5982

Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors

Author keywords

EGFR inhibitor; Quinoline 3 carbonitrile

Indexed keywords

4 (CYCLOPROPYLAMINO)QUINOLINE 3 CARBONITRILE DERIVATIVE; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; GEFITINIB; PELITINIB; UNCLASSIFIED DRUG;

EID: 34548833037     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.07.071     Document Type: Article
Times cited : (47)

References (14)
  • 13
    • 34548848420 scopus 로고    scopus 로고
    • note
    • v-src peptide, 1% DMSO, and 0.0098-10 μM testing compound. Assays were initiated with the addition of the ATP substrate. Data were fitted to the Dixon competitive inhibition equation using Grafit 5.0 (Erithacus Software).
  • 14
    • 34548830049 scopus 로고    scopus 로고
    • note
    • Cell-based EGFR autophosphorylation (Y1068) was performed with A431 cells in a 96-well format. Briefly, A431 cells (60,000 per well) were incubated at 37 °C overnight in 200 μL of Dulbecco's Modified Eagle's Medium (DMEM, GIBCOBRL, Cat#11995-073) containing 10% FBS. After removal of the medium, EGFR inhibitor in 100 μL DMEM was added and incubated for 60 min at 37 °C. Human EGF (40 ng/well) in DMEM was added and incubated for additional 20 min. Routine wash and 60 μL PIPA-2 buffer were added to lyse the cells. After centrifugation, the supernatant of the cell lysates was detected with ELISA kit for pY1068 according to the manufacturer's instruction (Biosource).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.