Discovery of potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 12, 2013, Pages 3531-3538

  Gunzner Toste, Janet ^a   Zhao, Guiling ^a   Bauer, Paul ^b   Baumeister, Timm ^b   Buckmelter, Alexandre J ^b   Caligiuri, Maureen ^b   Clodfelter, Karl H ^b   Fu, Bang ^c   Han, Bingsong ^b   Ho, Yen Ching ^b   Kley, Nikolai ^b   Liang, Xiaorong ^a   Liederer, Bianca M ^a   Lin, Jian ^b   Mukadam, Sophie ^a   O'Brien, Thomas ^a   Oh, Angela ^a   Reynolds, Dominic J ^b   Sharma, Geeta ^b   Skelton, Nicholas ^a   Smith, Chase C ^b   Sodhi, Jasleen ^a   Wang, Weiru ^a   Wang, Zhongguo ^b   Xiao, Yang ^a   Yuen, Po Wai ^c   Zak, Mark ^a   Zhang, Lei ^c   Zheng, Xiaozhang ^b   Bair, Kenneth W ^b   Dragovich, Peter S ^a   more..

^a GENENTECH INC   (United States)

^b Forma Therapeutics   (United States)

^c Pharmaron Beijing Co Ltd   (China)

Author keywords

CYP2C9; Cytochrome P450; NAMPT; Nicotinamide phosphoribosyltransferase; X ray crystal structure

Indexed keywords

CYTOCHROME P450 2C9; GLYCOSYLTRANSFERASE INHIBITOR; NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE; NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG EFFICACY; DRUG POTENCY; DRUG STRUCTURE; ENZYME ACTIVITY; ENZYME INHIBITION; IC 50; PROCESS OPTIMIZATION;

ANIMALS; ARYL HYDROCARBON HYDROXYLASES; HUMANS; MICE; MICE, INBRED BALB C; NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE; UREA;

EID: 84878114435     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.04.040     Document Type: Article

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