Discovery of 2-(6-{[(6-Fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex- 3-yl)- N -hydroxypyrimidine-5-carboxamide (CHR-3996), a class i selective orally active histone deacetylase inhibitor

Journal of Medicinal Chemistry

Volumn 53, Issue 24, 2010, Pages 8663-8678

  Moffat, David ^a   Patel, Sanjay ^a   Day, Francesca ^a   Belfield, Andrew ^a   Donald, Alastair ^a   Rowlands, Martin ^b   Wibawa, Judata ^b   Brotherton, Deborah ^a   Stimson, Lindsay ^b   Clark, Vanessa ^a   Owen, Jo ^a   Bawden, Lindsay ^a   Box, Gary ^b   Bone, Elisabeth ^a   Mortenson, Paul ^c   Hardcastle, Anthea ^b   Van Meurs, Sandra ^a   Eccles, Suzanne ^b   Raynaud, Florence ^b   Aherne, Wynne ^b  

^a Chroma Therapeutics Ltd   (United Kingdom)

^b INSTITUTE OF CANCER RESEARCH   (United Kingdom)

^c EVOTEC UK LTD   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

2 [6 [[(6 FLUOROQUINOLIN 2 YL)METHYL]AMINO]BICYCLO[3.1.0]HEX 3 YL] N HYDROXYPYRIMIDINE 5 CARBOXAMIDE; CHR 3996; HISTONE DEACETYLASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; CELL PROLIFERATION; COLORECTAL CANCER; CONTROLLED STUDY; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TISSUE LEVEL; ENZYME INHIBITION; HUMAN; HUMAN TISSUE; IC 50; MOUSE; NONHUMAN; XENOGRAFT;

ANIMALS; ANTINEOPLASTIC AGENTS; AZABICYCLO COMPOUNDS; CELL LINE, TUMOR; DOGS; DRUG SCREENING ASSAYS, ANTITUMOR; DRUG SYNERGISM; FEMALE; HISTONE DEACETYLASE INHIBITORS; HUMANS; MICE; MICE, NUDE; MICROSOMES, LIVER; MODELS, MOLECULAR; NEOPLASM TRANSPLANTATION; PYRIMIDINES; RATS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TISSUE DISTRIBUTION; TRANSPLANTATION, HETEROLOGOUS;

EID: 78650390271     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm101177s     Document Type: Article

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