A Combination Strategy to Inhibit Pim-1: Synergism between Noncompetitive and ATP-Competitive Inhibitors

ChemMedChem

Volumn 8, Issue 3, 2013, Pages 484-496

  Mori, Mattia ^a,b   Tintori, Cristina ^a   Christopher, Robert Selwyne Arul ^a   Radi, Marco ^a   Schenone, Silvia ^c   Musumeci, Francesca ^c   Brullo, Chiara ^c   Sanità, Patrizia ^d   DelleMonache, Simona ^d   Angelucci, Adriano ^d   Kissova, Miroslava ^e   Crespan, Emmanuele ^e   Maga, Giovanni ^e   Botta, Maurizio ^a,f  

^a UNIVERSITY OF SIENA   (Italy)

^b SAPIENZA UNIVERSITY OF ROME   (Italy)

^c UNIVERSITY OF GENOA   (Italy)

^d UNIVERSITY OF L'AQUILA   (Italy)

^e CNR   (Italy)

^f Temple University   (United States)

Author keywords

Cancer; Medicinal chemistry; Noncompetitive inhibition; Organic synthesis; Pim 1

Indexed keywords

2 AMINOTHIAZOLE DERIVATIVE; 4 ACETYL 3 HYDROXY 1 [2 (1H INDOL 3 YL)ETHYL] 5 (4 ISOPROPYLPHENYL) 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 3 HYDROXY 1 [2 (1H INDOL 3 YL)ETHYL] 5 [4 (TRIFLUOROMETHYL)PHENYL) 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 3 HYDROXY 1 [2 (1H INDOL 3 YL)ETHYL] 5 PHENYL 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 3 HYDROXY 1 [2 (5 METHOXY 1H INDOL 3 YL)ETHYL] 5 (2 PHENYLETHYL) 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 3 HYDROXY 1 [2 (5 METHOXY 1H INDOL 3 YL)ETHYL] 5 (3 PHENOXYOHENYL) 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 3 HYDROXY 1 [2 (5 METHOXY 1H INDOL 3 YL)ETHYL] 5 (4 METHOXYPHENYL) 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 3 HYDROXY 1 [2 (5 METHOXY 1H INDOL 3 YL)ETHYL] 5 (4 METHYLPHENYL) 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 3 HYDROXY 1 [2 (5 METHOXY 1H INDOL 3 YL)ETHYL] 5 (4 PIPERIDIN 1 YLPHENYL) 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 3 HYDROXY 1 [2 (5 METHOXY 1H INDOL 3 YL)ETHYL] 5 [4 (TRIFLUOROMETHYL)PHENYL] 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 3 HYDROXY 1 [2 (5 METHOXY 1H INDOL 3 YL)ETHYL] 5 PHENYL 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 3 HYDROXY 1 [2 1H INDOL 3 YL)ETHYL] 5 (2 PHENYLETHYL) 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 3 HYDROXY 1 [2 1H INDOL 3 YL)ETHYL] 5 (3 PHENOXYPHENYL) 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 3 HYDROXY 1 [2 1H INDOL 3 YL)ETHYL] 5 (4 PIPERIDIN 1 YLPHENYL) 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 3 HYDROXY 5 (4 ISOPROPYLPHENYL) 1 [2 (5 METHOXY 1H INDOL 3 YL)ETHYL] 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 5 (1,1' BIPHENYL 4 YL) 3 HYDROXY 1 [2 (1H INDOL 3 YL)ETHYL] 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 5 (1,1' BIPHENYL 4 YL) 3 HYDROXY 1 [2 (5 METHOXY 1H INDOL 3 YL)ETHYL] 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 5 (4 BROMOPHENYL) 3 HYDROXY 1 [2 (5 METHOXY 1H INDOL 3 YL)ETHYL] 1,5 DIHYDRO 2H PYRROL 2 ONE; 4 ACETYL 5 (4 BROMOPHENYL) 3 HYDROXY 1 [2 1H INDOL 3 YL)ETHYL]1,5 DIHYDRO 2H PYRROL 2 ONE; ADENOSINE TRIPHOSPHATASE COMPETITIVE INHIBITOR; ADENOSINE TRIPHOSPHATASE INHIBITOR; ADENOSINE TRIPHOSPHATE; ANTINEOPLASTIC AGENT; NONCOMPETITIVE ADENOSINE TRIPHOSPHATASE INHIBITOR; PACLITAXEL; PEPTIDE; PROTEIN KINASE PIM 1; UNCLASSIFIED DRUG;

ARTICLE; CANCER CELL CULTURE; CONTROLLED STUDY; DRUG MECHANISM; DRUG POTENTIATION; DRUG STRUCTURE; ENZYME INHIBITION; HUMAN; HUMAN CELL; PRIORITY JOURNAL; PROSTATE CANCER;

ADENOSINE TRIPHOSPHATE; ANTINEOPLASTIC AGENTS; BINDING SITES; BINDING, COMPETITIVE; CELL LINE, TUMOR; CELL SURVIVAL; CRYSTALLOGRAPHY, X-RAY; HUMANS; INDOLES; KINETICS; MOLECULAR DOCKING SIMULATION; PROTEIN BINDING; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; PROTO-ONCOGENE PROTEINS C-PIM-1; PYRROLES; RECOMBINANT PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES;

EID: 84874339477     PISSN: 18607179     EISSN: 18607187     Source Type: Journal    
DOI: 10.1002/cmdc.201200480     Document Type: Article

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