Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 24, 2014, Pages 5683-5687

  Fauber, Benjamin P ^a   Dragovich, Peter S ^a   Chen, Jinhua ^b   Corson, Laura B ^a   Ding, Charles Z ^b   Eigenbrot, Charles ^a   Labadie, Sharada ^a   Malek, Shiva ^a   Peterson, David ^a   Purkey, Hans E ^a   Robarge, Kirk ^a   Sideris, Steve ^a   Ultsch, Mark ^a   Wei, Binqing ^a   Yen, Ivana ^a   Yue, Qin ^a   Zhou, Aihe ^a  

^a GENENTECH INC   (United States)

^b WUXI APPTEC   (China)

Author keywords

LDHA; Tumor metabolism; X ray crystal structure

Indexed keywords

CYCLOPROPANE DERIVATIVE; LACTATE DEHYDROGENASE; LACTATE DEHYDROGENASE A; METHYL GROUP; PYRONE DERIVATIVE; UNCLASSIFIED DRUG; ENZYME INHIBITOR;

ANIMAL CELL; ARTICLE; BINDING SITE; CELL VIABILITY; CYCLIZATION; DRUG IDENTIFICATION; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; HYDROGEN BOND; IC50; IN VITRO STUDY; LIPOPHILICITY; MDCK CELL LINE; MOLECULAR DOCKING; NONHUMAN; PERMEABILITY; PLASMA PROTEIN BINDING; RAT; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; METABOLISM; SYNTHESIS;

BINDING SITES; CRYSTALLOGRAPHY, X-RAY; ENZYME INHIBITORS; HUMANS; L-LACTATE DEHYDROGENASE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PYRONES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84911870497     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2014.10.067     Document Type: Article

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