Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1

Journal of Medicinal Chemistry

Volumn 58, Issue 12, 2015, Pages 5053-5074

  Gazzard, Lewis ^a   Williams, Karen ^b   Chen, Huifen ^a   Axford, Lorraine ^b   Blackwood, Elizabeth ^a   Burton, Brenda ^b   Chapman, Kerry ^b   Crackett, Peter ^b   Drobnick, Joy ^a   Ellwood, Charles ^b   Epler, Jennifer ^a   Flagella, Michael ^a   Gancia, Emanuela ^b   Gill, Matthew ^b   Goodacre, Simon ^b   Halladay, Jason ^a   Hewitt, Joanne ^b   Hunt, Hazel ^b   Kintz, Samuel ^a   Lyssikatos, Joseph ^a   Macleod, Calum ^b   Major, Sarah ^b   Médard, Guillaume ^b   Narukulla, Raman ^b   Ramiscal, Judi ^a   Schmidt, Stephen ^a   Seward, Eileen ^b   Wiesmann, Christian ^a   Wu, Ping ^a   Yee, Sharon ^a   Yen, Ivana ^a   Malek, Shiva ^a   more..

^a GENENTECH INC   (United States)

^b CHARLES RIVER LABORATORIES   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

1,7 DIAZACARBAZOLE DERIVATIVE; 3 (1 METHYL 1H PYRAZOL 3 YL) 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 (1H IMIDAZOL 2 YL) 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 (2 HYDROXYPHENYL) 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 (4 MORPHOLINOPHENYL) 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 (ETHYLAMINO) 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 (FURAN 3 YL) 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 (PYRIDIN 3 YL) 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 (PYRIDIN 4 YL) 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 (THIOPHEN 2 YL) 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 HYDROXY 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 [3 (4 METHYLPIPERAZIN 1 YL)PHENYL] 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 [3 (HYDROXYMETHYL)PHENYL] 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 [4 (4 METHYLPIPERAZIN 1 YL)PHENYL] 9H PYRROLO[2,3 B:5,4 C' ]DIPYRIDINE 6 CARBONITRILE; 3 [4 (PIPERIDIN 1 YLMETHYL)PHENYL] 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 [4 [(2 OXA 7 AZASPIRO[3.5]NONAN 7 YL)METHYL]PHENYL] 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 [4 [(2,6 DIMETHYLPIPERIDIN 1 YL)METHYL]PHENYL] 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 [4 [(3,3 DIMETHYLPIPERIDIN 1 YL)METHYL]PHENYL] 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 [4 [(3,5 DIMETHYLPIPERIDIN 1 YL)METHYL]PHENYL] 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 3 [4 [(4,4 DIMETHYLPIPERIDIN 1 YL)METHYL]PHENYL] 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 6 CARBONITRILE 3 [4 (HYDROXYMETHYL)PHENYL] 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; 9H PYRROLO[2,3 B:5,4 C']DIPYRIDINE 6 CARBONITRILE; ACETYLCHOLINESTERASE; CARBAZOLE DERIVATIVE; CHECKPOINT KINASE 1; CHOLINESTERASE INHIBITOR; GEMCITABINE; N [3 (6 CYANO 9H PYRROLO[2,3 B:5,4 C']DIPYRIDIN 3 YL)PHENYL]ACETAMIDE; PROTEIN SERINE THREONINE KINASE INHIBITOR; UNCLASSIFIED DRUG; UNINDEXED DRUG; HETEROCYCLIC COMPOUND; PROTEIN KINASE; PROTEIN KINASE INHIBITOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; CRYSTAL STRUCTURE; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG CONFORMATION; DRUG EFFICACY; DRUG POTENCY; DRUG POTENTIATION; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; HUMAN CELL; HYDROGEN BOND; IN VITRO STUDY; IN VIVO STUDY; MOLECULAR DOCKING; MOUSE; NONHUMAN; PROCESS OPTIMIZATION; PROTEIN PHOSPHORYLATION; STRUCTURE ACTIVITY RELATION; TUMOR VOLUME; TUMOR XENOGRAFT; ANIMAL; CHEMICAL STRUCTURE; CHEMISTRY; DOG; ENZYMOLOGY; METABOLISM; NEOPLASMS; NUDE MOUSE; RAT; TUMOR CELL LINE; X RAY CRYSTALLOGRAPHY;

ACETYLCHOLINESTERASE; ANIMALS; AZA COMPOUNDS; CARBAZOLES; CELL LINE, TUMOR; CHOLINESTERASE INHIBITORS; CRYSTALLOGRAPHY, X-RAY; DOGS; HUMANS; MICE; MICE, NUDE; MODELS, MOLECULAR; NEOPLASMS; PROTEIN KINASE INHIBITORS; PROTEIN KINASES; RATS;

EID: 84933055970     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b00464     Document Type: Article

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