Discovery of 4-{4-[(3R)-3-methylmorpholin-4-yl]-6-[1-(methylsulfonyl) cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): A potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity

Journal of Medicinal Chemistry

Volumn 56, Issue 5, 2013, Pages 2125-2138

  Foote, Kevin M ^a   Blades, Kevin ^a   Cronin, Anna ^a   Fillery, Shaun ^a   Guichard, Sylvie S ^a   Hassall, Lorraine ^a   Hickson, Ian ^b   Jacq, Xavier ^b   Jewsbury, Philip J ^a   McGuire, Thomas M ^a   Nissink, J Willem M ^a   Odedra, Rajesh ^a   Page, Ken ^a   Perkins, Paula ^a   Suleman, Abid ^a   Tam, Kin ^a   Thommes, Pia ^a   Broadhurst, Rebecca ^a   Wood, Christine ^a  

^a ASTRAZENECA   (United Kingdom)

^b KuDOS Pharmaceuticals   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

4 [4 (3 METHYLMORPHOLIN 4 YL) 6 (1 (METHYLSULFONYL) CYCLOPROPYL)PYRIMIDIN 2 YL] 1H INDOLE; ANTINEOPLASTIC AGENT; ATR PROTEIN; AZ 20; MAMMALIAN TARGET OF RAPAMYCIN; PHOSPHATIDYLINOSITOL 3 KINASE; PIPERIDINE; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ALKYLATION; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER INHIBITION; CARCINOMA CELL; COLORECTAL CARCINOMA; CONTROLLED STUDY; DOWNSTREAM PROCESSING; DRUG EFFICACY; DRUG EXPOSURE; DRUG POTENCY; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME PHOSPHORYLATION; FEMALE; IMMUNOPRECIPITATION; IN VITRO STUDY; IN VIVO STUDY; LIPOPHILICITY; MONOTHERAPY; MOUSE; NONHUMAN; PERMEABILITY; REACTION OPTIMIZATION; XENOGRAFT;

ANIMALS; ANTINEOPLASTIC AGENTS; CELL CYCLE PROTEINS; CRYSTALLOGRAPHY, X-RAY; DRUG DISCOVERY; FEMALE; HELA CELLS; HUMANS; MICE; MODELS, MOLECULAR; MORPHOLINES; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; PYRIMIDINES; STRUCTURE-ACTIVITY RELATIONSHIP; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84875143334     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm301859s     Document Type: Article

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