Indole RSK inhibitors. Part 2: Optimization of cell potency and kinase selectivity

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 1, 2012, Pages 738-742

  Kirrane, Thomas M ^a   Boyer, Stephen J ^a,b   Burke, Jennifer ^a   Guo, Xin ^a   Snow, Roger J ^a   Soleymanzadeh, Lida ^a   Swinamer, Alan ^a   Zhang, Yunlong ^a   Madwed, Jeffery B ^a,c   Kashem, Mohammed ^a   Kugler, Stanley ^a   O'Neill, Margaret M ^a  

^a BOEHRINGER INGELHEIM PHARMACEUTICALS INC   (United States)

^b BRISTOL MYERS SQUIBB   (United States)

^c MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Kinase inhibitor; MAPKAP K1; RSK

Indexed keywords

1 OXO 2,3,4,5 TETRAHYDRO 1H [1,4]DIAZEPINO[1,2 A]INDOLE 8 CARBOXAMIDE DERIVATIVE; BIX 02565; CYTOCHROME P450 3A4; CYTOCHROME P450 INHIBITOR; INDOLE; S6 KINASE; UNCLASSIFIED DRUG;

ARTICLE; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; ENZYME ACTIVITY; ENZYME BINDING; ENZYME INHIBITION; HEART FAILURE; SOLUBILITY;

AMIDES; CHEMISTRY, PHARMACEUTICAL; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; HUMANS; INDOLES; INHIBITORY CONCENTRATION 50; MODELS, CHEMICAL; MOLECULAR CONFORMATION; NITROGEN; RIBOSOMAL PROTEIN S6 KINASES, 90-KDA; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84655170016     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.10.029     Document Type: Article

References (13)

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13. Inhibition of the phosphorylation of the transcription factor CREB (cAMP Response Element Binding) by RSK2 in cells was determined according to the method described in: Boyer, S.; Gao, A.; Guo, X.; Kirrane, T.; Sarko, C.; Snow, R.; Soleymanzadeh, F.; Zhang, Y. WO2011071716.