1253585-27-1Relevant articles and documents
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
, p. 7047 - 7063 (2013)
Novel small molecule inhibitors of heat shock protein 90 (Hsp90) were discovered with the help of a fragment based drug discovery approach (FBDD) and subsequent optimization with a combination of structure guided design, parallel synthesis and application of medicinal chemistry principles. These efforts led to the identification of compound 18 (NMS-E973), which displayed significant efficacy in a human ovarian A2780 xenograft tumor model, with a mechanism of action confirmed in vivo by typical modulation of known Hsp90 client proteins, and with a favorable pharmacokinetic and safety profile.
RESORCINOL DERIVATIVES AS HSP90 INHIBITORS
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Page/Page column 57, (2010/11/05)
The present invention relates to substituted resorcinol derivatives which inhibit the activity of Heat Shock Protein HSP90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, pharmaceutical compositions comprising them, methods of treating diseases and the pharmaceutical compositions comprising these compounds.