Discovery of pyrimidine benzimidazoles as Lck inhibitors: Part I

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 20, 2008, Pages 5618-5621

  Zhang, Guobao ^a   Ren, Pingda ^a   Gray, Nathanael S ^a   Sim, Taebo ^a   Liu, Yi ^a   Wang, Xia ^a   Che, Jianwei ^a   Tian, Shin Shay ^a   Sandberg, Mark L ^a   Spalding, Tracy A ^a   Romeo, Russell ^a   Iskandar, Maya ^a   Chow, Donald ^a   Martin Seidel, H ^a   Karanewsky, Donald S ^a   He, Yun ^a  

^a GENOMICS INSTITUTE OF THE NOVARTIS RESEARCH FOUNDATION   (United States)

Author keywords

Autoimmune disease; Kinase inhibitor; Lck inhibitor; Pyrimidine benzimidazoles; Transplantation rejection

Indexed keywords

4 AMINO 6 BENZIMIDAZOLE PYRIMIDINE DERIVATIVE; LCK TYROSINE KINASE INHIBITOR; PROTEIN KINASE LCK; PROTEIN TYROSINE KINASE; PYRIMIDINE BENZIMIDAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; DRUG DESIGN; DRUG SYNTHESIS; ENZYME INHIBITION; IC 50; MOLECULAR MODEL; NONHUMAN; REACTION OPTIMIZATION;

AUTOIMMUNE DISEASES; BENZIMIDAZOLES; CHEMISTRY, PHARMACEUTICAL; DRUG DESIGN; HUMANS; INHIBITORY CONCENTRATION 50; LYMPHOCYTE SPECIFIC PROTEIN TYROSINE KINASE P56(LCK); MODELS, CHEMICAL; MOLECULAR CONFORMATION; PROTEIN-TYROSINE KINASES; PYRIMIDINES; SOLUBILITY; SRC-FAMILY KINASES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 53449083913     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.08.104     Document Type: Article

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24. In a typical assay, transformed Ba/F3 cells were plated in 384-well plates (25,000 cells per well) and incubated with serial dilutions of inhibitor or DMSO for 48 h. Luciferase expression was used as a measure of cell proliferation/survival and was evaluated with the Bright-Glo Luciferase Assay System (Promega, Madison, WI).