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

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

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

Affiliation

Brasca MG; Nerviano Medical Sciences S.r.l., Oncology, Viale Pasteur 10, 20014 Nerviano, MI, Italy. Electronic address: gabriella.brasca@nervianoms.com.

Bioorg Med Chem ; 21(22): 7047-63, 2013 Nov 15.

Article in En | MEDLINE | ID: mdl-24100158

Subject(s)

Antineoplastic Agents/chemistry; Antineoplastic Agents/pharmacology; HSP90 Heat-Shock Proteins/antagonists & inhibitors; Isoxazoles/chemistry; Isoxazoles/pharmacology; Animals; Antineoplastic Agents/therapeutic use; Binding Sites; Biomarkers, Tumor/metabolism; Catalytic Domain; Cell Line, Tumor; Cell Survival/drug effects; Crystallography, X-Ray; Drug Design; Drug Evaluation, Preclinical; Female; HSP90 Heat-Shock Proteins/metabolism; Humans; Isoxazoles/therapeutic use; Mice; Mice, Inbred BALB C; Mice, Nude; Ovarian Neoplasms/drug therapy; Ovarian Neoplasms/metabolism; Ovarian Neoplasms/pathology; Protein Binding/drug effects; Structure-Activity Relationship; Transplantation, Heterologous

Key words

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

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Full text: 1 Database: MEDLINE Main subject: HSP90 Heat-Shock Proteins / Isoxazoles / Antineoplastic Agents Limits: Animals / Female / Humans Language: En Journal: Bioorg Med Chem Journal subject: BIOQUIMICA / QUIMICA Year: 2013 Type: Article

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