Conformational refinement of hydroxamate-based histone deacetylase inhibitors and exploration of 3-piperidin-3-ylindole analogues of dacinostat (LAQ824)

Journal of Medicinal Chemistry

Volumn 53, Issue 7, 2010, Pages 2952-2963

  Cho, Young Shin ^a   Whitehead, Lewis ^a   Li, Jianke ^a   Chen, Christine H T ^a   Jiang, Lei ^a   Vögtle, Markus ^b   Francotte, Eric ^b   Richert, Paul ^b   Wagner, Trixie ^b   Traebert, Martin ^b   Lu, Qiang ^a   Cao, Xueying ^a   Dumotier, Berengere ^b   Fejzo, Jasna ^a   Rajan, Srinivasan ^a   Wang, Ping ^a   Yan Neale, Yan ^a   Shao, Wenlin ^a   Atadja, Peter ^a   Shultz, Michael ^a  

^a NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

^b Werk Klybeck   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

3 [4 (3 (2 TERT BUTYL 1H INDOL 3 YL) PIPERIDIN 1 YLMETHYL) 3 FLUOROPHENYL] N HYDROXYACRYLAMIDE; 3 PIPERIDINE 3 YLINDOLE; 4 [N (2 HYDROXYETHYL) N [2 (3 INDOLYL)ETHYL]AMINOMETHYL]CINNAMOHYDROXAMIC ACID; HISTONE DEACETYLASE INHIBITOR; INDOLE; MOLECULAR SCAFFOLD; POTASSIUM CHANNEL HERG; UNCLASSIFIED DRUG;

ARTICLE; CELL ASSAY; CONFORMATION; CONTROLLED STUDY; DRUG BINDING; ENANTIOMER; HUMAN; HUMAN CELL; LIPOPHILICITY; RACEMIC MIXTURE; STRUCTURE ACTIVITY RELATION;

CELL LINE, TUMOR; CELL PROLIFERATION; HISTONE DEACETYLASE INHIBITORS; HISTONE DEACETYLASES; HUMANS; HYDROXAMIC ACIDS; INDOLES; INHIBITORY CONCENTRATION 50; MODELS, MOLECULAR; MOLECULAR CONFORMATION; STEREOISOMERISM;

EID: 77950582432     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm100007m     Document Type: Article

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