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Volumn 21, Issue 12, 2011, Pages 3788-3793

Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors

Author keywords

Anaplastic lymphoma kinase; Antitumor efficacy; Kinase inhibitors

Indexed keywords

ANAPLASTIC LYMPHOMA KINASE; ANTINEOPLASTIC AGENT; CRIZOTINIB; PROTEIN TYROSINE KINASE INHIBITOR; TETRACYCLIC COMPOUND; UNCLASSIFIED DRUG;

EID: 79957869630     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.04.020     Document Type: Article
Times cited : (34)

References (20)
  • 13
    • 79957868519 scopus 로고    scopus 로고
    • note
    • 2 using time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
  • 15
    • 79957817552 scopus 로고    scopus 로고
    • note
    • Cell growth inhibitory assay: KARPAS-299 cells were treated with various concentrations of assay compounds for 96 h. Cell growth inhibition was determined by cell counting kit-8 assay.
  • 16
    • 79957857008 scopus 로고    scopus 로고
    • note
    • Microsomal stability assay: 1 μM of each compound was incubated with human (or mouse) liver microsome (0.5 mg protein/mL) in 50 mM phosphate buffer (pH 7.4) containing 1 mM NADPH (the reduced form of nicotinamide adenine dinucleotide phosphate) at 37 °C for 30 min. After the enzyme reaction was terminated with the addition of a three-fold volume of acetonitrile, the reaction mixture was centrifuged at 1500 rpm for 10 min. The resultant supernatant was used as a test sample to measure the stability in human (or mouse) liver microsome by quantitating the compound in the sample using LC/MS.
  • 18
    • 79957857906 scopus 로고    scopus 로고
    • note
    • The quantity of enzyme and ATP and the kind of substrate and cation species added in each assay are given in Supplementary Table 1.
  • 19
    • 79957820693 scopus 로고    scopus 로고
    • note
    • 0 x 100, where W and W0 are the body weight on a specific experimental day and on the first day of treatment, respectively.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.