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Volumn 19, Issue 12, 2009, Pages 3344-3347

Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors

Author keywords

JNK; Kinase

Indexed keywords

AMIDE; PIPERAZINE DERIVATIVE; STRESS ACTIVATED PROTEIN KINASE; STRESS ACTIVATED PROTEIN KINASE INHIBITOR;

EID: 65949111743     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.03.086     Document Type: Article
Times cited : (26)

References (31)
  • 23
    • 50049116341 scopus 로고    scopus 로고
    • For the review of reported JNK inhibitors:
    • For the review of reported JNK inhibitors:. LoGrasso P., and Kamenecka T. Mini-Rev. Med. Chem. 8 (2008) 755
    • (2008) Mini-Rev. Med. Chem. , vol.8 , pp. 755
    • LoGrasso, P.1    Kamenecka, T.2
  • 24
    • 65949083487 scopus 로고    scopus 로고
    • note
    • 50s for JNKs 1 and 3 were determined using HTRF. Briefly, final assay concentrations of JNK1, JNK3, biotinylated-ATF2 and ATP were 0.1 nM, 0.3 nM, 0.4 nM and 1 μM, respectively. In each assay the phosphor-Thr71-ATF-2 product was detected using a Europium-cryptate labeled anti-phospho-Thr71-ATF-2 antibody. Streptavidin-allophycocyanin-XL was used as the acceptor. A 10-point dose-response curve for each compound was generated in duplicate and data was fit to a four parameter logistic.
  • 25
    • 65949094495 scopus 로고    scopus 로고
    • note
    • Most compounds containing the bromofuran moiety had microsome stabilities for rat ≤5 min.
  • 26
    • 65949095327 scopus 로고    scopus 로고
    • note
    • 50 values were determined using a four parameter logistic and a 10-point dilution curve for each of the inhibitors covering four orders of magnitude of inhibitor concentration.
  • 29
    • 65949114982 scopus 로고    scopus 로고
    • note
    • Crystallographic coordinates of JNK3 complexed with 4g have been deposited at the Protein Data Bank (www.rcsb.org/) with PDB ID code 3FV8.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.