Identification, characterization and initial hit-to-lead optimization of a series of 4-arylamino-3-pyridinecarbonitrile as protein kinase C theta (PKCθ) inhibitors

Journal of Medicinal Chemistry

Volumn 51, Issue 19, 2008, Pages 5958-5963

  Cole, Derek C ^a   Asselin, Magda ^a   Brennan, Agnes ^b   Czerwinski, Robert ^b   Ellingboe, John W ^a   Fitz, Lori ^b   Greco, Rita ^b   Huang, Xinyi ^b   Joseph McCarthy, Diane ^b,c   Kelly, Michael F ^a   Kirisits, Matthew ^a   Lee, Julie ^b   Li, Yuanhong ^b   Morgan, Paul ^b   Stock, Joseph R ^a   Tsao, Désirée H H ^b   Wissner, Allan ^a   Yang, Xiaoke ^b   Chaudhary, Divya ^b  

^a WYETH RESEARCH   (United States)

^b PFIZER INC   (United States)

^c ASTRAZENECA   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

3 PYRIDINECARBONITRILE DERIVATIVE; 4 (3 BROMOPHENYLAMINO) 5 (3,4 DIMETHOXYPHENYL) 3 PYRIDINECARBONITRILE; 5 (3,4 DIMETHOXYPHENYL) 4 (1H INDOL 5 YLAMINO) 3 PYRIDINECARBONITRILE; INTERLEUKIN 2; PROTEIN KINASE B; PROTEIN KINASE C; PROTEIN KINASE C EPSILON; PROTEIN KINASE C INHIBITOR; PROTEIN KINASE C THETA; PROTEIN SERINE THREONINE KINASE; TYROSINE; UNCLASSIFIED DRUG;

ARTICLE; CYTOKINE PRODUCTION; DRUG STRUCTURE; ENZYME ACTIVITY; HIGH THROUGHPUT SCREENING; PROTON NUCLEAR MAGNETIC RESONANCE; SPLEEN CELL; T LYMPHOCYTE ACTIVATION;

ANIMALS; CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; FEMALE; INDOLES; INTERLEUKIN-2; ISOENZYMES; MICE; MICE, INBRED C57BL; MICE, KNOCKOUT; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NITRILES; PROTEIN KINASE C; PROTEIN KINASE INHIBITORS; PYRIDINES; SPLEEN; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; T-LYMPHOCYTES;

EID: 53549089928     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm800214a     Document Type: Article

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