Structure-based design of novel 2-amino-6-phenyl-pyrimido[5′, 4′:5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): Synthesis, SAR, and in vivo anti-inflammatory activity

Journal of Medicinal Chemistry

Volumn 51, Issue 6, 2008, Pages 1637-1648

  Martin, Matthew W ^a   Newcomb, John ^a   Nunes, Joseph J ^a   Boucher, Christina ^a   Chai, Lilly ^a   Epstein, Linda F ^a   Faust, Theodore ^a   Flores, Sylvia ^a   Gallant, Paul ^a   Gore, Anu ^a   Gu, Yan ^a   Hsieh, Faye ^a   Huang, Xin ^a   Kim, Joseph L ^a   Middleton, Scot ^a   Morgenstern, Kurt ^a   Oliveira dos Santos, Antonio ^a   Patel, Vinod F ^a   Powers, David ^a   Rose, Paul ^a   Tudor, Yanyan ^a   Turci, Susan M ^a   Welcher, Andrew A ^a   Zack, Debra ^a   Zhao, Huilin ^a   Zhu, Li ^a   Zhu, Xiaotian ^a   Ghiron, Chiara ^b   Ermann, Monika ^b   Johnston, David ^b   Saluste, Carl Gustaf Pierre ^b   more..

^a AMGEN INC   (United States)

^b EVOTEC UK LTD   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

2 AMINO 6 PHENYL PYRIMIDO[5''4':5,6]PYRIMIDO[1,2 A]BENZIMIDAZOL 5(6H) ONE DERIVATIVE; 6 (2,6 DIMETHYLPHENYL) 2 ((4 (4 METHYL 1 PIPERAZINYL)PHENYL)AMINOPYRIMIDO[5',4':5,6]PYRIMIDO [1,2 A]BENZIMIDAZOL 5(6H) ONE; PROTEIN KINASE LCK; UNCLASSIFIED DRUG;

ANIMAL MODEL; ARTICLE; CELL MATURATION; CONTROLLED STUDY; DRUG ACTIVITY; DRUG HALF LIFE; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME ACTIVITY; IN VIVO STUDY; MOUSE; NATURAL KILLER CELL; NONHUMAN; RAT; SINGLE DRUG DOSE; X RAY CRYSTALLOGRAPHY;

ADMINISTRATION, ORAL; ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; ARTHRITIS; BENZIMIDAZOLES; CRYSTALLOGRAPHY, X-RAY; DISEASE MODELS, ANIMAL; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; ENZYME ACTIVATION; FEMALE; INJECTIONS, INTRADERMAL; INTERLEUKIN-2; LYMPHOCYTE SPECIFIC PROTEIN TYROSINE KINASE P56(LCK); MALE; MICE; MICE, INBRED BALB C; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN KINASE INHIBITORS; PYRIMIDINONES; RATS; RATS, INBRED LEW; RATS, SPRAGUE-DAWLEY; REPRODUCIBILITY OF RESULTS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; T-LYMPHOCYTES;

EID: 41149118544     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm701095m     Document Type: Article

References (57)

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