Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor

ACS Medicinal Chemistry Letters

Volumn 7, Issue 2, 2016, Pages 134-138

  Mitchell, Lorna H ^a   Boriack Sjodin, P Ann ^a   Smith, Sherri ^a   Thomenius, Michael ^a   Rioux, Nathalie ^a   Munchhof, Michael ^a   Mills, James E ^a   Klaus, Christine ^a   Totman, Jennifer ^a   Riera, Thomas V ^a   Raimondi, Alejandra ^a   Jacques, Suzanne L ^a   West, Kip ^a   Foley, Megan ^a   Waters, Nigel J ^a   Kuntz, Kevin W ^a   Wigle, Tim J ^a,b   Scott, Margaret Porter ^a,c   Copeland, Robert A ^a   Smith, Jesse J ^a   Chesworth, Richard ^a   more..

^a EPIZYME INC   (United States)

^b Genentech Inc ^*  (United States)

^c GENENTECH INC   (United States)

Author keywords

KMT; methyltransferase; oncology; oxindole; SMYD3; tool compound

Indexed keywords

EPZ 030456; EPZ 031686; HISTONE LYSINE METHYLTRANSFERASE; OXINDOLE; SET AND MYND DOMAIN CONTAINING 3; SMALL MOLECULE TRANSPORT AGENT; SULFAMIDE DERIVATIVE; SULFONAMIDE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; APPARENT PERMEABILITY; AREA UNDER THE CURVE; ARTICLE; CRYSTAL STRUCTURE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG EXCRETION; DRUG METABOLISM; DRUG PENETRATION; DRUG POTENCY; DRUG SCREENING; HYDROGEN BOND; HYDROPHOBICITY; IC50; IN VITRO STUDY; IN VIVO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; METABOLIC STABILITY; MOUSE; NONHUMAN; PRIORITY JOURNAL; TIME TO MAXIMUM PLASMA CONCENTRATION; VOLUME OF DISTRIBUTION AT STEADY-STATE;

EID: 84958982766     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/acsmedchemlett.5b00272     Document Type: Article

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