1247003-58-2Relevant academic research and scientific papers
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.
Efficient Microwave-Assisted Synthesis of Sonogashira-Coupled Perylene Monoimide Derivatives: Impact of Electron-Donating Groups on Optoelectronic Properties
Sharma, Vikas,Chandra, Falguni,Sahoo, Dhananjaya,Koner, Apurba L.
, p. 6901 - 6905 (2017/12/26)
An efficient microwave-assisted Sonogashira-coupling protocol for the synthesis of peri-functionalized perylene monoimide dye derivatives was developed. This method was found to be significantly faster than the conventional coupling method and provided pr
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.
KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME
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Page/Page column 206-207, (2010/11/03)
The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: 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.
