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Volumn 21, Issue 8, 2011, Pages 2264-2269

Design and synthesis of isoquinolines and benzimidazoles as RAF kinase inhibitors

Author keywords

Benzimidazole; Isoquinoline; RAF kinase

Indexed keywords

BENZIMIDAZOLE DERIVATIVE; HETEROCYCLIC AMINE; ISOQUINOLINE DERIVATIVE; MITOGEN ACTIVATED PROTEIN KINASE; RAF PROTEIN; SORAFENIB;

EID: 79953281702     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.02.108     Document Type: Article
Times cited : (20)

References (44)
  • 22
    • 79953278716 scopus 로고    scopus 로고
    • note
    • The structural information about the B-RAF kinase domain (SWID: P15056) is used as surrogate for the kinase domain of c-RAF (RAF1) (SWID: P04049). The residue identity is 81.7%. The hinge region has the identical sequence.
  • 27
    • 79953273381 scopus 로고    scopus 로고
    • note
    • CCDC GOLD version 4.1 with default screening parameters and without any constraints. The binding mode was validated by the successful reproduction of the crystal structure via redocking, which is considered as validation for the docking of similar structures.
  • 33
    • 79953277178 scopus 로고    scopus 로고
    • Chem. Abstr. 2005, 143, 286297.
    • (2005) Chem. Abstr. , vol.143 , pp. 286297
  • 34
    • 79953279223 scopus 로고    scopus 로고
    • note
    • In a final reaction volume of 25 μL, human c-RAF (5-10 mU, Millipore) was incubated with 25 mM Tris pH 7.5, 0.02 mM EGTA, 0.66 mg/mL myelin basic protein, 10 mM Mg acetate and [γ-33P-ATP] (specific activity approx. 500 cpm/pmol). The reaction was initiated by the addition of the MgATP mix. After incubation for 40 min at room temperature, the reaction was stopped by the addition of 3% phosphoric acid solution. The reaction was then spotted onto a P30 filtermat and washed prior to drying and scintillation counting. All measurements were performed in duplicates.
  • 35
    • 79953283206 scopus 로고    scopus 로고
    • Unpublished results
    • Unpublished results.
  • 43
    • 79953270026 scopus 로고    scopus 로고
    • Chem. Abstr. 2005, 143, 266924.
    • (2005) Chem. Abstr. , vol.143 , pp. 266924
  • 44
    • 65249098311 scopus 로고    scopus 로고
    • Kinetic solubility of the compounds was determined according to B. Hoelke, S. Gieringer, M. Arlt, and C. Saal Anal. Chem. 81 2009 3165 (HPLC method) using phosphate buffer (50 mM). 10f: 4.2 μg/ml; 10m: <1 μg/ml; 10n: 16.4 μg/ml; 19c: 12.4 μg/ml; 19n: 82.7 μg/ml; 19q: 81.2 μg/ml
    • (2009) Anal. Chem. , vol.81 , pp. 3165
    • Hoelke, B.1    Gieringer, S.2    Arlt, M.3    Saal, C.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.