Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase

Journal of Medicinal Chemistry

Volumn 50, Issue 9, 2007, Pages 2213-2224

  Mortlock, Andrew A ^a   Foote, Kevin M ^a   Heron, Nicola M ^a   Jung, Frédéric H ^a   Pasquet, Georges ^a   Lohmann, Jean Jacques M ^a   Warin, Nicolas ^a   Renaud, Fabrice ^a   De Savi, Chris ^a   Roberts, Nicola J ^a   Johnson, Trevor ^a   Dousson, Cyril B ^a   Hill, George B ^a   Perkins, David ^a   Hatter, Glenn ^a   Wilkinson, Robert W ^a   Wedge, Stephen R ^a   Heaton, Simon P ^a   Odedra, Rajesh ^a   Keen, Nicholas J ^a   Crafter, Claire ^a   Brown, Elaine ^a   Thompson, Katherine ^a   Brightwell, Stephen ^a   Khatri, Liz ^a   Brady, Madeleine C ^a   Kearney, Sarah ^a   McKillop, David ^a   Rhead, Steve ^a   Parry, Tony ^a   Green, Stephen ^a   more..

^a ASTRAZENECA   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

AURORA A KINASE; AURORA B KINASE; AZD 1152; PHOSPHATE; PRODRUG; PYRAZOLE DERIVATIVE; QUINAZOLINE DERIVATIVE; RECOMBINANT ENZYME; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CONTINUOUS INFUSION; CONTROLLED STUDY; DRUG SAFETY; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME ASSAY; ENZYME INHIBITION; FEMALE; IN VIVO STUDY; MALE; MOUSE; NONHUMAN; PHENOTYPE; RAT;

ANIMALS; ANTINEOPLASTIC AGENTS; CELL DIVISION; CELL LINE, TUMOR; CYTOCHROME P-450 ENZYME SYSTEM; DRUG SCREENING ASSAYS, ANTITUMOR; ETHER-A-GO-GO POTASSIUM CHANNELS; FEMALE; HISTONES; HUMANS; MALE; MICE; MICE, NUDE; PHOSPHORIC ACID ESTERS; PHOSPHORYLATION; PRODRUGS; PROTEIN BINDING; PROTEIN-SERINE-THREONINE KINASES; PYRAZOLES; QUINAZOLINES; RATS; RECOMBINANT PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSPLANTATION, HETEROLOGOUS;

EID: 34247603906     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm061335f     Document Type: Article

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29. Cell activity data is given for a single cell line (SW620). Activity for compounds in this pyrazole series in a range of human tumor cell lines will be reported elsewhere.
30. While a number of different prodrug strategies were considered, only the phosphate ester approach is described here.
31. a of ethylamine is 10.72 and that of 2-methoxyethyl ethylamine is 9.40.
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