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Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 21, 2012, Pages 6671-6676

Discovery of phosphoinositide 3-kinases (PI3K) p110β isoform inhibitor 4-[2-hydroxyethyl(1-naphthylmethyl)amino]-6-[(2S)-2-methylmorpholin-4-yl]-1H- pyrimidin-2-one, an effective antithrombotic agent without associated bleeding and insulin resistance

(11) Giordanetto, Fabrizio a Wållberg, Andreas a Ghosal, Saswati a Iliefski, Tommy a Cassel, Johan a Yuan, Zhong Qing a Von Wachenfeldt, Henrik a Andersen, Soren M a Inghardt, Tord a Tunek, Anders a Nylander, Sven a

a ASTRAZENECA R AND D (Sweden)

Author keywords

Anti thrombotic agent; Fragment based; Inhibitor; Insulin resistance; p110 ; Phosphoinositide 3 kinase; PI3K; Thromboembolism

Indexed keywords

4 [ 2 HYDROXYETHYL( 1 NAPHTHYLMETHYL)AMINO] 6 [ 2 METHYLMORPHOLIN 4 YL] 1H PYRIMIDIN 2 ONE; ANTICOAGULANT AGENT; AZD 6482; INSULIN; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; PROTEIN P110; PROTEIN P110 ALPHA; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANTICOAGULATION; ARTICLE; BLEEDING; CONTROLLED STUDY; DOG; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG SAFETY; DRUG SELECTIVITY; DRUG SOLUBILITY; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; IN VIVO STUDY; INSULIN BLOOD LEVEL; INSULIN RESISTANCE; LIVER MICROSOME; NONHUMAN; RAT; THROMBOCYTE AGGREGATION;

1-PHOSPHATIDYLINOSITOL 4-KINASE; ANIMALS; BLEEDING TIME; BLOOD PLATELETS; CLASS I PHOSPHATIDYLINOSITOL 3-KINASES; DOGS; DRUG DISCOVERY; FIBRINOLYTIC AGENTS; INHIBITORY CONCENTRATION 50; INSULIN RESISTANCE; MOLECULAR STRUCTURE; MORPHOLINES; PROTEIN ISOFORMS; PYRIMIDINONES; RATS;

CANIS FAMILIARIS; RATTUS;

EID: 84867582164 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2012.08.102 Document Type: Article

Times cited : (15)

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