Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 24, 2008, Pages 6352-6356

  Kopecky, David J ^a   Hao, Xiaolin ^a   Chen, Yi ^a   Fu, Jiasheng ^a   Jiao, XianYun ^a   Jaen, Juan C ^b   Cardozo, Mario G ^a   Liu, Jinsong ^a   Wang, Zhulun ^a   Walker, Nigel P C ^a   Wesche, Holger ^a   Li, Shyun ^a   Farrelly, Ellyn ^a   Xiao, Shou Hua ^a   Kayser, Frank ^a  

^a AMGEN INC   (United States)

^b ChemoCentryx Inc   (United States)

Author keywords

ACK1; Cancer; Kinase inhibitor; Pyrazolo 3,4, d pyrimidine 3,6 diamine; SAR

Indexed keywords

1H PYRAZOLO[3,4 D]PYRIMIDINE 3,6 DIAMINE DERIVATIVE; PROTEIN TYROSINE KINASE; PROTEIN TYROSINE KINASE INHIBITOR; TYROSINE KINASE ACK1; UNCLASSIFIED DRUG; ACK1 PROTEIN, HUMAN; DIAMINE; ENZYME INHIBITOR; PYRAZOLE DERIVATIVE; PYRIMIDINE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG IDENTIFICATION; DRUG STRUCTURE; DRUG SYNTHESIS; HIGH THROUGHPUT SCREENING; MALE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; ANIMAL; CHEMICAL MODEL; CHEMISTRY; CONFORMATION; DRUG ANTAGONISM; IC 50; METHODOLOGY; SPRAGUE DAWLEY RAT; SYNTHESIS; X RAY CRYSTALLOGRAPHY;

ANIMALS; CHEMISTRY, PHARMACEUTICAL; CRYSTALLOGRAPHY, X-RAY; DIAMINES; DRUG DESIGN; ENZYME INHIBITORS; INHIBITORY CONCENTRATION 50; MALE; MODELS, CHEMICAL; MOLECULAR CONFORMATION; PROTEIN-TYROSINE KINASES; PYRAZOLES; PYRIMIDINES; RATS; RATS, SPRAGUE-DAWLEY; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 56249103764     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.10.092     Document Type: Article

References (17)

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10. Unpublished results.
11. is were generated by fitting the dose response data to the Morrison equation.
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