Preparation and optimization of new 4-(2-(indolin-1-yl)-2-oxoethyl)-2- morpholinothiazole-5-carboxylic acid and amide derivatives as potent and selective PI3Kβ inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 6, 2014, Pages 1506-1510

  Certal, Victor ^a   Halley, Frank ^a   Virone Oddos, Angela ^a   Filoche Rommé, Bruno ^a   Carry, Jean Christophe ^a   Gruss Leleu, Florence ^a   Bertin, Luc ^a   Guizani, Houlfa ^a   Pilorge, Fabienne ^a   Richepin, Patrick ^a   Karlsson, Andreas ^a   Charrier, Véronique ^a   Abecassis, Pierre Yves ^a   Vincent, Loic ^a   Nicolas, Jean Paul ^a   Lengauer, Christoph ^a   Garcia Echeverria, Carlos ^a   Schio, Laurent ^a  

^a SANOFI   (France)

Author keywords

pAKT; PI3K ; PTEN; Thiazole

Indexed keywords

4 (2 (INDOLIN 1 YL) 2 OXOETHYL) 2 MORPHOLINOTHIAZOLE 5 CARBOXYLIC ACID; AMIDE; CARBOXYLIC ACID; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; THIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BINDING SITE; BIOCHEMISTRY; DRUG STRUCTURE; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; MALE; NONHUMAN; RAT;

PAKT; PI3KΒ; PTEN; THIAZOLE;

AMIDES; ANIMALS; BINDING SITES; CACO-2 CELLS; CARBOXYLIC ACIDS; HUMANS; INDOLES; MALE; MOLECULAR DOCKING SIMULATION; PERMEABILITY; PHOSPHATIDYLINOSITOL 3-KINASES; PROTEIN ISOFORMS; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; PROTO-ONCOGENE PROTEINS C-AKT; RATS; RATS, SPRAGUE-DAWLEY; THIAZOLES;

EID: 84895788977     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2014.02.004     Document Type: Article

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