1247003-58-2Relevant articles and documents
Fragment-Based Drug Design Facilitated by Protein-Templated Click Chemistry: Fragment Linking and Optimization of Inhibitors of the Aspartic Protease Endothiapepsin
Mondal, Milon,Unver, M. Yagiz,Pal, Asish,Bakker, Matthijs,Berrier, Stephan P.,Hirsch, Anna K. H.
, p. 14826 - 14830 (2016)
There is an urgent need for the development of efficient methodologies that accelerate drug discovery. We demonstrate that the strategic combination of fragment linking/optimization and protein-templated click chemistry is an efficient and powerful method that accelerates the hit-identification process for the aspartic protease endothiapepsin. The best binder, which inhibits endothiapepsin with an IC50value of 43 μm, represents the first example of triazole-based inhibitors of endothiapepsin. Our strategy could find application on a whole range of drug targets.
KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME
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Page/Page column 103-104, (2011/10/31)
The invention is directed to a compound represented by the following structural formula pharmaceutically acceptable salts thereof: (I). Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.