Structure-based discovery of BM-957 as a potent small-molecule inhibitor of Bcl-2 and Bcl-xL capable of achieving complete tumor regression

Journal of Medicinal Chemistry

Volumn 55, Issue 19, 2012, Pages 8502-8514

  Chen, Jianfang ^a   Zhou, Haibin ^a   Aguilar, Angelo ^a   Liu, Liu ^a   Bai, Longchuan ^a   McEachern, Donna ^a   Yang, Chao Yie ^a   Meagher, Jennifer L ^a   Stuckey, Jeanne A ^a   Wang, Shaomeng ^a  

^a UNIVERSITY OF MICHIGAN   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 (4 CHLOROPHENYL) 1 ETHYL 4 [3 [4 [4 [4 [4 (4 HYDROXYPIPERID 1 YL) 1 (PHENYLTHIO)BUTAN 2 YLAMINO) 3 (TRIFLUOROMETHYLSULFONYL)PHENYLSULFONAMIDO]PHENYL]PIPERAZIN 1 YL]PHENYL] 2 METHYL 1H PYRROLE 3 CARBOXYLIC ACID; 5 (4 CHLOROPHENYL) 4 [3 [4 [4 [4 [4 (4 HYDROXYPIPERIDIN 1 YL) 1 (PHENYLTHIO)BUTAN 2 YLAMINO) 3 (TRIFLUOROMETHYLSULFONYL) PHENYLSULFONAMIDO]PHENYL]PIPERAZIN 1 YL]PHENYL] 1 ISOPROPYL 2 METHYL 1H PYRROLE 3 CARBOXYLIC ACID; 5 (4 CHLOROPHENYL) 4 [3 [4 [4 [4 [4 (4 HYDROXYPIPERIDIN 1 YL) 1 (PHENYLTHIO)BUTAN 2 YLAMINO) 3 (TRIFLUOROMETHYLSULFONYL)PHENYLSULFONAMIDO]PHENYL]PIPERAZIN 1 YL]PHENYL] 1,2 DIMETHYL 1H PYRROLE 3 CARBOXYLIC ACID; ANTINEOPLASTIC AGENT; BM 957; PROTEIN BCL 2; PROTEIN BCL XL; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CANCER INHIBITION; DRUG DESIGN; DRUG STRUCTURE; HUMAN; HUMAN CELL; LUNG CANCER; MOUSE; NONHUMAN; TUMOR REGRESSION; TUMOR XENOGRAFT;

ANIMALS; ANTINEOPLASTIC AGENTS; BCL-X PROTEIN; CARCINOMA, NON-SMALL-CELL LUNG; CELL LINE, TUMOR; CRYSTALLOGRAPHY, X-RAY; DRUG SCREENING ASSAYS, ANTITUMOR; HUMANS; LUNG NEOPLASMS; MICE; MICE, SCID; NEOPLASM TRANSPLANTATION; PROTEIN CONFORMATION; PROTO-ONCOGENE PROTEINS C-BCL-2; PYRROLES; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES; TUMOR BURDEN;

EID: 84867341788     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm3010306     Document Type: Article

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