Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90)

Bioorganic and Medicinal Chemistry

Volumn 21, Issue 22, 2013, Pages 7047-7063

  Brasca, Maria Gabriella ^a   Mantegani, Sergio ^a   Amboldi, Nadia ^a   Bindi, Simona ^a   Caronni, Dannica ^a   Casale, Elena ^a   Ceccarelli, Walter ^a   Colombo, Nicoletta ^a   De Ponti, Anna ^a   Donati, Daniele ^a   Ermoli, Antonella ^a   Fachin, Gabriele ^a   Felder, Eduard R ^a   Ferguson, Ronald D ^a   Fiorelli, Claudio ^a   Guanci, Marco ^a   Isacchi, Antonella ^a   Pesenti, Enrico ^a   Polucci, Paolo ^a   Riceputi, Laura ^a   Sola, Francesco ^a   Visco, Carlo ^a   Zuccotto, Fabio ^a   Fogliatto, Gianpaolo ^a   more..

^a NERVIANO MEDICAL SCIENCES   (Italy)

Author keywords

Anti cancer agents; Fragment based drug discovery; Tumor cell proliferation inhibition

Indexed keywords

3 (5 CHLORO 2,4 DIHYDROXYPHENYL) N ETHYL 4 (4 METHOXYPHENYL) 5 PYRAZOLECARBOXAMIDE; 5 (4 CHLOROPHENOXY) 4 (ISOXAZOL 5 YL)BENZENE 1,3 DIOL; 5 [2 (4 CHLOROPHENOXY) 4,6 DIHYDROXYPHENYL] N ETHYISOXAZOLE 3 CARBOXAMIDE; 5 [2 [4 (DIMETHYLAMINO)PHENOXY] 4,6 DIHYDROXYPHENYL] N (1 METHYLPIPERIDIN 4 YL)ISOXAZOLE 3 CARBOXAMIDE; 5 [2 [4 (DIMETHYLAMINO)PHENOXY] 4,6 DIHYDROXYPHENYL] N [1 (1,4 DIOXASPIRO[4.5]DEC 8 YL)PIPERIDIN 4 YL]ISOXAZOLE 3 CARBOXAMIDE; 5 [2,4 DIHYDROXY 6 (4 NITROPHENOXY)PHENYL] N (1 METHYLPIPERIDIN 4 YL)ISOXAZOLE 3 CARBOXAMIDE; 5 [2,4 DIHYDROXY 6 (4 NITROPHENOXY)PHENYL] N (1,2,2,6,6 PENTAMETHYLPIPERIDIN 4 YL)ISOXAZOLE 3 CARBOXAMIDE; 5 [2,4 DIHYDROXY 6 (4 NITROPHENOXY)PHENYL] N (2 HYDROXYETHYL)ISOXAZOLE 3 CARBOXAMIDE; 5 [2,4 DIHYDROXY 6 (4 NITROPHENOXY)PHENYL] N (2 METHYOXYETHYL)ISOXAZOLE 3 CARBOXAMIDE; 5 [2,4 DIHYDROXY 6 (4 NITROPHENOXY)PHENYL] N (PIPERIDIN 4 YLMETHYL)ISOXAZOLE 3 CARBOXAMIDE TRIFLUOROACETATE; 5 [2,4 DIHYDROXY 6 (4 NITROPHENOXY)PHENYL] N [(1 METHYLPIPERIDIN 4 YL)METHYL]ISOXAZOLE 3 CARBOXAMIDE; 5 [2,4 DIHYDROXY 6 (4 NITROPHENOXY)PHENYL] N [3 (DIMETHYLAMINO)PROPYL]ISOXAZOLE 3 CARBOXAMIDE; 5 [2,4 DIHYDROXY 6 (4 NITROPHENOXY)PHENYL] N,N DIMETHYLISOXAZOLE 3 CARBOXAMIDE; 5 [2,4 DIHYDROXY 6 [4 (PROPAN 2 YLAMINO)PHENOXY]PHENYL] N (1 METHYLPIPERIDIN 4 YL)ISOXAZOLE 3 CARBOXAMIDE; EPIDERMAL GROWTH FACTOR RECEPTOR 2; HEAT SHOCK PROTEIN 70; HEAT SHOCK PROTEIN 90; HEAT SHOCK PROTEIN 90 INHIBITOR; LUMINESPIB; MITOGEN ACTIVATED PROTEIN KINASE; N (1 ACETYLPIPERIDIN 4 YL) 5 [2,4 DIHYDROXY 6 (4 NITROPHENOXY)PHENYL]ISOZAXOLE 3 CARBOXAMIDE; N (1 BENZYLPIPERIDIN 4 YL) 5 [2,4 DIHYDROXY 6 (4 NITROPHENOXY)PHENYL]ISOZAXOLE 3 CARBOXAMIDE; N (CYCLOHEXYLMETHYL) 5 [2,4 DIHYDROXY 6 (4 NITROPHENOXY)PHENYL]ISOXAZOLE 3 CARBOXAMIDE; N BENZYL 5 [2,4 DIHYDROXY 6 (4 NITROPHENOXY)PHENYL]ISOXAZOLE 3 CARBOXAMIDE; N CYCLOHEXYL 5 [2,4 DIHYDROXY 6 (4 NITROPHENOXY)PHENYL]ISOXAZOLE 3 CARBOXAMIDE; N ETHYL 5 [2 HYDROXY 6 (4 NITROPHENOXY)PHENYL]ISOXAZOLE 3 CARBOXAMIDE; N ETHYL 5 [4 HYDROXY 2 (4 NITROPHENOXY)PHENYL]ISOXAZOLE 3 CARBOXAMIDE; NMS E973; PROTEIN KINASE B; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CANCER CELL CULTURE; DRUG CLEARANCE; DRUG DESIGN; DRUG DISTRIBUTION; DRUG DOSE COMPARISON; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG MECHANISM; DRUG POTENCY; DRUG SAFETY; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; HUMAN; HUMAN CELL; IN VIVO STUDY; MOUSE; MULTIPLE CYCLE TREATMENT; NONHUMAN; OVARY CANCER; PH; PROTEIN DEGRADATION; STRUCTURE ACTIVITY RELATION; TUMOR XENOGRAFT;

ANTI-CANCER AGENTS; FRAGMENT BASED DRUG DISCOVERY; TUMOR CELL PROLIFERATION INHIBITION;

ANIMALS; ANTINEOPLASTIC AGENTS; BINDING SITES; CATALYTIC DOMAIN; CELL LINE, TUMOR; CELL SURVIVAL; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; FEMALE; HSP90 HEAT-SHOCK PROTEINS; HUMANS; ISOXAZOLES; MICE; MICE, INBRED BALB C; MICE, NUDE; OVARIAN NEOPLASMS; PROTEIN BINDING; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSPLANTATION, HETEROLOGOUS; TUMOR MARKERS, BIOLOGICAL;

EID: 84885857466     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2013.09.018     Document Type: Article

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