Discovery of 8-Membered Ring Sulfonamides as Inhibitors of Oncogenic Mutant Isocitrate Dehydrogenase 1

ACS Medicinal Chemistry Letters

Volumn 7, Issue 10, 2016, Pages 944-949

  Law, Jason M ^a,b   Stark, Sebastian C ^a   Liu, Ke ^a   Liang, Norah E ^a,b   Hussain, Mahmud M ^a,b,c   Leiendecker, Matthias ^a,b   Ito, Daisuke ^a   Verho, Oscar ^a,b   Stern, Andrew M ^a   Johnston, Stephen E ^a   Zhang, Yan Ling ^a   Dunn, Gavin P ^d   Shamji, Alykhan F ^a   Schreiber, Stuart L ^a,b,c  

^a BROAD INSTITUTE OF MIT AND HARVARD   (United States)

^b HARVARD UNIVERSITY   (United States)

^c HOWARD HUGHES MEDICAL INSTITUTE   (United States)

^d WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

2 hydroxyglutarate; allele selective probe; AML; BRD2879; cancer; diversity oriented synthesis; glioma; high throughput screening; isocitrate dehydrogenase; small molecule probe

Indexed keywords

2 HYDROXYGLUTARIC ACID; BRD 2879; ISOCITRATE DEHYDROGENASE 1; ISOCITRATE DEHYDROGENASE INHIBITOR; N [2 CYCLOHEXYLAMINO 1 (2 METHYLPHENYL) 2 OXOETHYL] N (3 FLUOROPHENYL) 2 METHYL 1H IMIDAZOLE 1 ACETAMIDE; REDUCED NICOTINAMIDE ADENINE DINUCLEOTIDE PHOSPHATE; SULFONAMIDE; UNCLASSIFIED DRUG;

ALLELE; ARTICLE; DRUG SOLUBILITY; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; IN VITRO STUDY; MOLECULAR INTERACTION; PHARMACOKINETICS; PLASMA PROTEIN BINDING; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION;

EID: 84991490246     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/acsmedchemlett.6b00264     Document Type: Article

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