1073973-23-5Relevant articles and documents
Identification of novel HSP90α/β isoform selective inhibitors using structure-based drug design. demonstration of potential utility in treating CNS disorders such as huntington's disease
Ernst, Justin T.,Neubert, Timothy,Liu, Michael,Sperry, Samuel,Zuccola, Harmon,Turnbull, Amy,Fleck, Beth,Kargo, William,Woody, Lisa,Chiang, Peggy,Tran, Dao,Chen, Weichao,Snyder, Phillip,Alcacio, Timothy,Nezami, Azin,Reynolds, James,Alvi, Khisal,Goulet, Lance,Stamos, Dean
, p. 3382 - 3400 (2014/05/20)
A structure-based drug design strategy was used to optimize a novel benzolactam series of HSP90α/β inhibitors to achieve >1000-fold selectivity versus the HSP90 endoplasmic reticulum and mitochondrial isoforms (GRP94 and TRAP1, respectively). Selective HS
HSP90 MODULATING COMPOUNDS, COMPOSITIONS, METHODS AND USES
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Page/Page column 65; 66, (2011/04/24)
The invention relates to therapeutic compounds which bind to HSP90, said compounds containing a benzamide group bound to a tricyclic condensed ring system via the nitrogen atom of a pyrrole located in the center of the condensed system. The compounds disclosed herein bind HSP90 and alter the chaperoning capability of HSP90 proteins. Intermediate benzonitrile compounds which are precursors to the benzamide compounds are also disclosed. The invention also relates to pharmaceutical compositions comprising these compounds, and methods of treating diseases and disorders such as cancer, autoimmune diseases and other diseases.