Discovery and optimization of sulfonyl acrylonitriles as selective, covalent inhibitors of protein phosphatase methylesterase-1

Journal of Medicinal Chemistry

Volumn 54, Issue 14, 2011, Pages 5229-5236

  Bachovchin, Daniel A ^a   Zuhl, Andrea M ^a   Speers, Anna E ^a   Wolfe, Monique R ^a   Weerapana, Eranthie ^a   Brown, Steven J ^a   Rosen, Hugh ^a   Cravatt, Benjamin F ^a  

^a SCRIPPS RESEARCH INSTITUTE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 (4 FLUOROPHENYLSULFONYL) 3 [1 (PHENYLSULFONYL) 1H PYRROL 2 YL]ACRYLONITRILE; 2 (METHYLSULFONYL) 3 (1H PYRROL 2 YL)ACRYLONITRILE; 2 (METHYLSULFONYL) 3 (4 NITROPHENYL)ACRYLONITRILE; 2 (METHYLSULFONYL) 3 [1 (PHENYLSULFONYL) 1H PYRROL 2 YL]PROP 2 EN 1 AMINE; 2 (METHYLSULFONYL) 3 [1 (PHENYLSULFONYL) 1H PYRROL 2 YL]PROPANE NITRILE; 2 (METHYLSULFONYL) 3 [1 [(4 NITROPHENYL)SULFONYL] 1H PYRROL 2 YL]ACRYLONITRILE; 2 (METHYLSULFONYL) 3 [1 [(PERFLUOROPHENYL)SULFONYL] 1H PYRROL 2 YL]ACRYLONITRILE; 2 (METHYLSULFONYL) 3 PHENYLACRYLONITRILE; 2 (PHENYLSULFONYL) 3 (1H PYRROL 2 YL)ACRYLONITRILE; 2 (PHENYLSULFONYL) 3 [1 (PHENYLSULFONYL) 1H PYRROL 2 YL]ACRYLONITRILE; 2 (TERT BUTYLSULFONYL) 3 (1H PYRROL 2 YL)ACRYLONITRILE; 2 (TERT BUTYLSULFONYL) 3 [1 (PHENYLSULFONYL) 1H PYRROL 2 YL]ACRYLONITRILE; 2 [(1H PYRROL 2 YL)METHYLENE]MALONONITRILE; 2 [(4 FLUOROPHENYL)SULFONYL] 3 (1H PYRROL 2 YL)ACRYLONITRILE; 2 [2,2 BIS(METHYLSULFONYL)VINYL] 1 (PHENYLSULFONYL) 1H PYRROLE; 2 [2,2 BIS(METHYLSULFONYL)VINYL] 1H PYRROLE; 2 [[1 (PHENYLSULFONYL) 1H PYRROL 2 YL]METHYLENE]MALONONITRILE; 3 [1 (4 CHLOROPHENYLSULFONYL) 1H PYRROL 2 YL] 2 (METHYLSULFONYL)ACRYLONITRILE; 3 [2 [2 (TERT BUTYLSULFONYL) 2 CYANOVINYL] 1H PYRROL 1 YL SULFONYL]BENZONITRILE; 3 [2 [2 CYANO 2 (4 FLUOROPHENYLSULFONYL)VINYL] 1H PYRROL 1 YLSULFONYL]BENZONITRILE; 3 [2 [2 CYANO 2 (METHYLSULFONYL)VINYL] 1H PYRROL 1 YLSULFONYL]BENZONITRILE; 4 [2 [2 CYANO 2 (METHYLSULFONYL)VINYL] 1H PYRROL 1 YLSULFONYL]BENZONITRILE; ACRYLONITRILE; AMZ 30; PHOSPHATASE METHYLESTERASE 1; PHOSPHOPROTEIN PHOSPHATASE 2A; PROTEIN INHIBITOR; PROTEIN PHOSPHATASE METHYLESTERASE 1 INHIBITOR; SULFONYL ACRYLONITRILE INHIBITOR; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ARTICLE; CONTROLLED STUDY; DEMETHYLATION; DRUG DEVELOPMENT; ENZYME INACTIVATION; ENZYME INHIBITION; FLUORESCENCE; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IC 50; METHYLATION; POLARIZATION; PROTEIN BINDING; PROTEIN FUNCTION;

ACRYLONITRILE; CARBOXYLIC ESTER HYDROLASES; CELL LINE; HUMANS; PROTEOME; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES; SULFONES;

EID: 79960622162     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm200502u     Document Type: Article

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