Optimization of a series of dipeptides with a P3 β-neopentyl asparagine residue as non-covalent inhibitors of the chymotrypsin-like activity of human 20S proteasome

MedChemComm

Volumn 3, Issue 6, 2012, Pages 710-719

  Blackburn, Christopher ^a   Barrett, Cynthia ^a   Blank, Jonathan L ^a   Bruzzese, Frank J ^a   Bump, Nancy ^a   Dick, Lawrence R ^a   Fleming, Paul ^a   Garcia, Khristofer ^a   Hales, Paul ^a   Jones, Matthew ^a   Liu, Jane X ^a   Nagayoshi, Masayuki ^a   Sappal, Darshan S ^a   Sintchak, Michael D ^a   Tsu, Christopher ^a   Xia, Cindy ^a   Zhou, Xiansi ^a   Gigstad, Kenneth M ^a  

^a MILLENNIUM PHARMACEUTICALS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ASPARAGINE; BORONIC ACID DERIVATIVE; BORTEZOMIB; CHYMOTRYPSIN; DIPEPTIDE; N [3 (3 TERT BUTYL 1,2,4 OXADIAZOL 5 YL) 1 [1 (4 METHYLBENZYLAMINO) 1 OXO 4 PHENYLBUTAN 2 YLAMINO] 1 OXOPROPAN 2 YL] 5 METHYLISOXAZOLE 3 CARBOXAMIDE; N1 [1 (4 METHYLBENZYLAMINO) 1 OXO 4 PHENYLBUTAN 2 YL] 2 (5 METHYLISOXAZOLE 3 CARBOXAMIDO) N4 NEOPENTYLSUCCINAMIDE; PROTEASOME; PROTEASOME INHIBITOR; UNCLASSIFIED DRUG;

ANTIPROLIFERATIVE ACTIVITY; ARTICLE; CONTROLLED STUDY; DRUG MECHANISM; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; HYDROPHOBICITY; IN VITRO STUDY; MOLECULAR INTERACTION; PRIORITY JOURNAL; PROCESS OPTIMIZATION;

EID: 84878088921     PISSN: 20402503     EISSN: 20402511     Source Type: Journal    
DOI: 10.1039/c2md20060k     Document Type: Article

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