Novel peptidyl aryl vinyl sulfones as highly potent and selective inhibitors of cathepsins L and B

ChemMedChem

Volumn 5, Issue 9, 2010, Pages 1556-1567

  Mendieta, Laura ^a   Picó, Anna ^b   Tarragó, Teresa ^a   Teixidó, Meritxell ^a   Castillo, Marcos ^b   Rafecas, Llorenç ^c   Moyano, Albert ^b   Giralt, Ernest ^a,b  

^a INSTITUTE FOR RESEARCH IN BIOMEDICINE   (Spain)

^b UNIVERSITY OF BARCELONA   (Spain)

^c ENANTIA SL   (Spain)

Author keywords

Aryl vinyl sulfones; Cathepsins; Cysteine proteases; Enzymes; Medicinal chemistry

Indexed keywords

4 METHYL N [ 1 [ 1 (NAPHTHALEN 1 YL) 3 (PHENYLSULFONYL) ALLYLAMINO] 1 OXO 3 PHENYLPROPAN 2 YL]PIPERAZINE 1 CARBOXAMIDE; 4 METHYL N [ 1 OXO 3 PHENYL 1 [ 1 PHENYL 3 (PHENYLSULFONYL)ALLYLAMINO]PROPAN 2 YL]PIPERAZINE 1 CARBOXAMIDE; 4 METHYL N [ 4 METHYL 1 [ 1 (NAPHTHALEN 1 YL) 3 (PHENYLSULFONYL)ALLYLAMINO] 1 OXOPENTAN 2 YL]PIPERAZINE 1 CARBOXAMIDE; 4 METHYL N [ 4 METHYL 1 [ 1 (NAPHTHALEN 2 YL) 3 (PHENYLSULFONYL)ALLYLAMINO] 1 OXOPENTAN 2 YL]PIPERAZINE 1 CARBOXAMIDE; 4 METHYL N [ 4 METHYL 1 OXO 1 [ 1 PHENYL 3 (PHENYLSULFONYL)ALLYLAMINO]PENTAN 2 YL]PIPERAZINE 1 CARBOXAMIDE; CATHEPSIN B; CATHEPSIN L; CYSTEINE PROTEINASE INHIBITOR; N 1 OXO 3 PHENYL 1 [ 1 PHENYL 3 (PHENYLSULFONYL)ALLYLAMINO]PROPAN 2 YL)MORPHOLINE 4 CARBOXAMIDE; N [ 1 (2,4,6 TRIMETHYLPHENYL) 3 (PHENYLSULFONYL)ALLYL] 2 (4 METHYLPIPERAZIN 1 YL) 3 PHENYLPROPANAMIDE; N [ 1 (2,4,6 TRIMETHYLPHENYL) 3 (PHENYLSULFONYL)ALLYL] 2 MORPHOLINO 3 PHENYLPROPANAMIDE; N [ 1 (2,4,6 TRIMETHYLPHENYL) 3 (PHENYLSULFONYL)ALLYL] 4 METHYL 2 (4 METHYLPIPERAZIN 1 YL)PENTANAMIDE; N [ 1 (2,4,6 TRIMETHYLPHENYL) 3 (PHENYLSULFONYL)ALLYL] 4 METHYL 2 MORPHOLINOPENTANAMIDE; N [ 1 [ 1 (BIPHENYL 4 YL) 3 (PHENYLSULFONYL)ALLYLAMINO] 1 OXO 3 PHENYLPROPAN 2 YL]MORPHOLINE 4 CARBOXAMIDE; N [ 1 [ 1 (BIPHENYL 4 YL) 3 (PHENYLSULFONYL)ALLYLAMINO] 4 METHYL 1 OXOPENTAN 2 YL]MORPHOLINE 4 CARBOXAMIDE; N [ 1 [ 1 (NAPHTHALEN 2 YL) 3 (PHENYLSULFONYL)ALLYLAMINO] 1 OXO 3 PHENYLPROPAN 2 YL)MORPHOLINE 4 CARBOXAMIDE; N [ 1 [1 (BIPHENYL 4 YL) 3 (PHENYLSULFONYL)ALLYLAMINO] 1 OXO 3 PHENYLPROPAN 2 YL] 4 METHYLPIPERAZINE 1 CARBOXAMIDE; N [ 1 [1 (NAPHTHALEN 1 YL) 3 (PHENYLSULFONYL)ALLYLAMINO] 1 OXO 3 PHENYLPROPAN 2 YL]MORPHOLINE 4 CARBOXAMIDE; N [ 4 METHYL 1 [ 1 (NAPHTHALEN 1 YL) 3 (PHENYLSULFONYL) ALLYLAMINO] 1 OXOPENTAN 2 YL]MORPHOLINE 4 CARBOXAMIDE; N [ 4 METHYL 1 [ 1 (NAPHTHALEN 2 YL) 3 (PHENYLSULFONYL) ALLYLAMINO] 1 OXOPENTAN 2 YL]MORPHOLINE 4 CARBOXAMIDE; N [ 4 METHYL 1 OXO 1 [ 1 PHENYL 3 (PHENYLSULFONYL)ALLYL AMINO]PENTAN 2 YL]MORPHOLINE 4 CARBOXAMIDE; SULFONE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; DRUG DESIGN; DRUG INHIBITION; DRUG MECHANISM; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME ACTIVITY; PRIORITY JOURNAL; SOLID PHASE SYNTHESIS; STRUCTURE ACTIVITY RELATION;

BINDING SITES; CATHEPSIN B; CATHEPSIN L; COMPUTER SIMULATION; HUMANS; PROTEASE INHIBITORS; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONES;

EID: 77956406470     PISSN: 18607179     EISSN: 18607187     Source Type: Journal    
DOI: 10.1002/cmdc.201000109     Document Type: Article

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