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Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56(Lck).
Chen, Ping; Norris, Derek; Iwanowicz, Edwin J; Spergel, Steven H; Lin, James; Gu, Henry H; Shen, Zhongqi; Wityak, John; Lin, Tai-An; Pang, Suhong; De Fex, Henry F; Pitt, Sidney; Shen, Ding Ren; Doweyko, Arthur M; Bassolino, Donna A; Roberge, Jacques Y; Poss, Michael A; Chen, Bang-Chi; Schieven, Gary L; Barrish, Joel C.
Affiliation
  • Chen P; Department of Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543, USA. ping.chen@bms.com
Bioorg Med Chem Lett ; 12(10): 1361-4, 2002 May 20.
Article in En | MEDLINE | ID: mdl-11992777
ABSTRACT
We have identified a novel series of 1,5-imidazoquinoxalines as inhibitors of Lck with excellent potency (IC50s<5 nM) as well as good cellular activity against T-cell proliferation (IC50s<1 microM). Structure-activity studies demonstrate the requirement for the core heterocycle in addition to an optimal 2,6-disubstituted aniline group.
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Collection: 01-internacional Database: MEDLINE Main subject: Quinoxalines / Src-Family Kinases / Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / Enzyme Inhibitors / Imidazoles Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2002 Document type: Article Affiliation country: United States
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Collection: 01-internacional Database: MEDLINE Main subject: Quinoxalines / Src-Family Kinases / Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / Enzyme Inhibitors / Imidazoles Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2002 Document type: Article Affiliation country: United States