Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization

Journal of Medicinal Chemistry

Volumn 58, Issue 3, 2015, Pages 1281-1297

  Zhao, Lele ^a   Wang, Yingqing ^a   Cao, Danyan ^a   Chen, Tiantian ^a   Wang, Qi ^a   Li, Yanlian ^a   Xu, Yechun ^a   Zhang, Naixia ^a   Wang, Xin ^a   Chen, Danqi ^a   Chen, Lin ^a   Chen, Yue Lei ^a   Xia, Guangxin ^b   Shi, Zhe ^c   Liu, Yu Chih ^c   Lin, Yijyun ^c   Miao, Zehong ^a   Shen, Jingkang ^a   Xiong, Bing ^a  

^a SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

^b Central Research Institute of Shanghai Pharmaceutical Holding Co   (China)

^c Shanghai ChemPartner Co Ltd   (China)

Author keywords

[No Author keywords available]

Indexed keywords

1 (3 BROMO 4 METHYL 5 NITROPHENYL)ETHANONE; 2 AMINO N CYCLOPENTYL 5 (2 OXO 2,3 DIHYDROTHIAZOL 4 YL)BENZENESULFONAMIDE; 2 CHLORO N CYCLOPENTYL 5 (2 OXO 2,3 DIHYDROTHIAZOL 4 YL)BENZENESULFONAMIDE; 3 (2 BROMOACETYL) N CYCLOPENTYLBENZENESULFONAMIDE; 3 (2 OXO 2,3 DIHYDROTHIAZOL 4 YL) N (TETRAHYDROFURAN 3 YL)BENZENESULFONAMIDE; 3 (2 OXO 2,3 DIHYDROTHIAZOL 4 YL) N [(TETRAHYDROFURAN 2 YL)METHYL]BENZENESULFONAMIDE; 3 (2 OXO 2,3 DIHYDROTHIAZOL 4 YL) N [2 (THIOPHEN 2 YL)ETHYL]BENZENESULFONAMIDE; 5 (2 BROMOACETYL) N CYCLOPENTYL 2 METHYLBENZENESULFONAMIDE; 5 (2 BROMOACETYL) N CYCLOPENTYL 2 NITROBENZENESULFONAMIDE; 5 ACETYL 2 METHYLBENZENE 1 SULFONYL CHLORIDE; 5 ACETYL 2 NITROBENZENE 1 SULFONYL CHLORIDE; 5 ACETYL N CYCLOPENTYL 2 METHYLBENZENESULFONAMIDE; 5 ACETYL N CYCLOPENTYL 2 NITROBENZENESULFONAMIDE; ANTINEOPLASTIC AGENT; BENZENESULFONAMIDE DERIVATIVE; BROMODOMAIN INHIBITOR; MYC PROTEIN; N (4 AMINOPHENYL) 3 (2 OXO 2,3 DIHYDROTHIAZOL 4 YL) BENZENESULFONAMIDE; N (4 METHOXYPHENYL) 3 (2 OXO 2,3 DIHYDROTHIAZOL 4 YL)BENZENESULFONAMIDE; N (5 ACETYL 2 NITROPHENYL)ACETAMIDE; N (ISOXAZOL 3 YL) 3 (2 OXO 2,3 DIHYDROTHIAZOL 4 YL) BENZENESULFONAMIDE; N BENZYL 3 (2 OXO 2,3 DIHYDROTHIAZOL 4 YL)BENZENESULFONAMIDE; N CYCLOHEXYL 3 (2 OXO 2,3 DIHYDROTHIAZOL 4 YL) BENZENESULFONAMIDE; N CYCLOPENTYL 2 FLUORO 5 (2 OXO 2,3 DIHYDROTHIAZOL 4 YL)BENZENESULFONAMIDE; N CYCLOPENTYL 2 METHOXY 5 (2 OXO 2,3 DIHYDROTHIAZOL 4 YL)BENZENESULFONAMIDE; N CYCLOPENTYL 2 METHYL 5 (2 OXO 2,3 DIHYDROTHIAZOL 4 YL)BENZENESULFONAMIDE; N CYCLOPENTYL 2 NITRO 5 (2 OXO 2,3 DIHYDROTHIAZOL 4 YL)BENZENESULFONAMIDE; N CYCLOPENTYL 3 (2 OXO 2,3 DIHYDROTHIAZOL 4 YL) BENZENESULFONAMIDE; N CYCLOPROPYL 3 (2 OXO 2,3 DIHYDROTHIAZOL 4 YL)BENZENESULFONAMIDE; UNCLASSIFIED DRUG; UNINDEXED DRUG; BRD4 PROTEIN, HUMAN; NUCLEAR PROTEIN; THIAZOLIDINE DERIVATIVE; TRANSCRIPTION FACTOR;

ARTICLE; CANCER CELL; CARBON NUCLEAR MAGNETIC RESONANCE; CELL PROLIFERATION; COLON CANCER; CONTROLLED STUDY; DOWN REGULATION; DRUG BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; HYDROGEN BOND; LIQUID CHROMATOGRAPHY; ONCOGENE C MYC; PROTEIN EXPRESSION; PROTON NUCLEAR MAGNETIC RESONANCE; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG DEVELOPMENT; DRUG EFFECTS; DRUG SCREENING; HT 29 CELL LINE; SYNTHESIS; TUMOR CELL CULTURE; X RAY CRYSTALLOGRAPHY;

ANTINEOPLASTIC AGENTS; CELL PROLIFERATION; CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; DRUG SCREENING ASSAYS, ANTITUMOR; HT29 CELLS; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NUCLEAR PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLIDINES; TRANSCRIPTION FACTORS; TUMOR CELLS, CULTURED;

EID: 84922822753     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501504k     Document Type: Article

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