Synthesis and structure-activity relationship studies of small molecule disruptors of EWS-FLI1 interactions in Ewing's sarcoma

Journal of Medicinal Chemistry

Volumn 57, Issue 24, 2014, Pages 10290-10303

  Tosso, Perrer N ^a,b   Kong, Yali ^a,b   Scher, Lauren ^b   Cummins, Ryan ^b   Schneider, Jeffrey ^b   Rahim, Said ^b   Holman, K Travis ^c   Toretsky, Jeffrey ^b   Wang, Kan ^a   Üren, Aykut ^b   Brown, Milton L ^a,b  

^a GEORGETOWN UNIVERSITY MEDICAL CENTER   (United States)

^b GEORGETOWN UNIVERSITY   (United States)

^c GEORGETOWN UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 HYDROXY 3 [2 (4 METHOXYPHENYL) 2 OXOETHYL] 4,7 DIMETHYLINDOLIN 2 ONE; 3 HYDROXY 3 [2 (4 METHOXYPHENYL) 2 OXOETHYL]INDOLIN 2 ONE; 3 HYDROXY 4,7 DIMETHOXY 3 [2 (4 METHOXYPHENYL) 2 OXOETHYL]INDOLIN 2 ONE; 4 CHLORO 3 HYDROXY 3 [2 (4 METHOXYPHENYL) 2 OXOETHYL]INDOLIN 2 ONE; 4 CHLOROINDOLINE 2,3 DIONE; 4 [2 (4,7 DICHLORO 3 HYDROXY 2 OXOINDOLIN 3 YL)ACETYL]BENZONITRILE; 4,7 DICHLORO 3 HYDROXY 3 (2 OXO 2 PHENYLETHYL) 1,3 DIHYDROINDOL 2 ONE; 4,7 DICHLORO 3 HYDROXY 3 [2 (2 METHOXYPHENYL) 2 OXOETHYL]INDOLIN 2 ONE; 4,7 DICHLORO 3 HYDROXY 3 [2 (3 METHOXYPHENYL) 2 OXOETHYL]INDOLIN 2 ONE; 4,7 DICHLORO 3 HYDROXY 3 [2 (4 IODOYPHENYL 2 OXOETHYL)] 1,3 DIHYDROINDOL 2 ONE; 4,7 DICHLORO 3 HYDROXY 3 [2 OXO 2 (2,3,4 TRIMETHOXYPHENYL)ETHYL]INDOLIN 2 ONE; 4,7 DICHLORO 3 HYDROXY 3 [2 OXO 2 [4 (TRIFLUOROMETHYL) PHENYL]ETHYL]INDOLIN 2 ONE; 4,7 DICHLORO 3 HYDROXYL 3 (2 OXO 2 P TOLYLETHYL) 1,3 DIHYDROINDOL 2 ONE; 4,7 DICHLORO 3 [2 (2,3 DIMETHOXYPHENYL) 2 OXOETHYL] 3 HYDROXYINDOLIN 2 ONE; 4,7 DICHLORO 3 [2 (2,4 DIMETHOXYPHENYL) 2 OXOETHYL] 3 HYDROXYINDOLIN 2 ONE; 4,7 DICHLORO 3 [2 (3,5 DIMETHOXYPHENYL) 2 OXOETHYL] 3 HYDROXYINDOLIN 2 ONE; 4,7 DICHLORO 3 [2 (4 ETHOXYPHENYL) 2 OXOETHYL] 3 HYDROXYINDOLIN 2 ONE; 4,7 DICHLORO 3 [2 (4 FLUOROPHENYL) 2 OXOETHYL)] 3 HYDROXYL 1,3 DIHYDROINDOL 2 ONE; 4,7 DIFLUORO 3 HYDROXY 3 [2 (4 METHOXYPHENYL) 2 OXOETHYL]INDOLIN 2 ONE; 4,7 DIFLUOROINDOLINE 2,3 DIONE; 4,7 DIMETHOXYINDOLINE 2,3 DIONE; 5 CHLORO 3 HYDROXY 3 [2 (4 METHOXYPHENYL) 2 OXOETHYL]INDOLIN 2 ONE; 5 CHLOROINDOLINE 2,3 DIONE; 5,6 DICHLORO 3 HYDROXY 3 [2 (4 METHOXYPHENYL) 2 OXOETHYL]INDOLIN 2 ONE; 5,6 DICHLOROINDOLINE 2,3 DIONE; 7 CHLORO 3 HYDROXY 3 [2 (4 METHOXYPHENYL) 2 OXOETHYL]INDOLIN 2 ONE; ANTINEOPLASTIC AGENT; EWS FLI1 PROTEIN; HYBRID PROTEIN; UNCLASSIFIED DRUG; UNINDEXED DRUG; 4,7-DICHLORO-3-(2-(4-(DIMETHYLAMINO)PHENYL)-2-OXOETHYL)-3-HYDROXYINDOLIN-2-ONE; ANILINE DERIVATIVE; EWS-FLI FUSION PROTEIN; INDOLE DERIVATIVE; LUCIFERASE; ONCOPROTEIN; RNA BINDING PROTEIN EWS; TRANSCRIPTION FACTOR FLI 1;

ANTIPROLIFERATIVE ACTIVITY; ARTICLE; BINDING AFFINITY; BINDING ASSAY; CARBON NUCLEAR MAGNETIC RESONANCE; CELL PROLIFERATION ASSAY; CELL SCREENING; CONTROLLED STUDY; DRUG SYNTHESIS; EWING SARCOMA; HUMAN; HUMAN CELL; HUMAN CELL CULTURE; HYDROGEN BOND; LUCIFERASE ASSAY; PROTEIN INTERACTION; PROTON NUCLEAR MAGNETIC RESONANCE; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; X RAY CRYSTALLOGRAPHY; ANTAGONISTS AND INHIBITORS; BONE NEOPLASMS; CELL PROLIFERATION; CHEMICAL STRUCTURE; DRUG EFFECTS; GENE EXPRESSION REGULATION; METABOLISM; PATHOLOGY; SARCOMA, EWING; SYNTHESIS; TUMOR CELL CULTURE;

ANILINE COMPOUNDS; ANTINEOPLASTIC AGENTS; BONE NEOPLASMS; CELL PROLIFERATION; CRYSTALLOGRAPHY, X-RAY; GENE EXPRESSION REGULATION, NEOPLASTIC; HUMANS; INDOLES; LUCIFERASES; MODELS, MOLECULAR; MOLECULAR STRUCTURE; ONCOGENE PROTEINS, FUSION; PROTO-ONCOGENE PROTEIN C-FLI-1; RNA-BINDING PROTEIN EWS; SARCOMA, EWING; STRUCTURE-ACTIVITY RELATIONSHIP; TUMOR CELLS, CULTURED;

EID: 84920150099     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501372p     Document Type: Article

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