Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H- pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases

Journal of Medicinal Chemistry

Volumn 56, Issue 5, 2013, Pages 2059-2073

  Addie, Matt ^a   Ballard, Peter ^a   Buttar, David ^a   Crafter, Claire ^a   Currie, Gordon ^a   Davies, Barry R ^a   Debreczeni, Judit ^a   Dry, Hannah ^a   Dudley, Philippa ^a   Greenwood, Ryan ^a   Johnson, Paul D ^a   Kettle, Jason G ^a   Lane, Clare ^a   Lamont, Gillian ^a   Leach, Andrew ^a   Luke, Richard W A ^a   Morris, Jeff ^a   Ogilvie, Donald ^a,b   Page, Ken ^a   Pass, Martin ^a   Pearson, Stuart ^a   Ruston, Linette ^a   more..

^a ASTRAZENECA   (United Kingdom)

^b UNIVERSITY OF MANCHESTER   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINO N [(1S) 1 (4 CHLOROPHENYL) 3 HYDROXYPROPYL] 1 (7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)PIPERIDINE 4 CARBOXAMIDE; ANTINEOPLASTIC AGENT; AZD 5363; POTASSIUM CHANNEL HERG; PROTEIN SERINE THREONINE KINASE INHIBITOR; UNCLASSIFIED DRUG;

ALKYLATION; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; BREAST CANCER; CANCER INHIBITION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFECT; DRUG HALF LIFE; DRUG METABOLISM; DRUG PROTEIN BINDING; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG STRUCTURE; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; HUMAN; HUMAN CELL; IN VIVO STUDY; MOUSE; NONHUMAN; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; TUMOR XENOGRAFT; X RAY CRYSTALLOGRAPHY;

ADMINISTRATION, ORAL; CELL LINE, TUMOR; FEMALE; HUMANS; INHIBITORY CONCENTRATION 50; MODELS, MOLECULAR; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-AKT; PYRIMIDINES; PYRROLES; STRUCTURE-ACTIVITY RELATIONSHIP; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84875184123     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm301762v     Document Type: Article

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