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Publication detail

Novel potential proteasome inhibitor based on tripeptide scaffold

Authors: Dušek Jan | Imramovský Aleš

Year: 2014

Type of publication: ostatní - přednáška nebo poster

Page from-to: nestránkováno

Titles:

Language	Name	Abstract	Keywords
eng	Novel potential proteasome inhibitor based on tripeptide scaffold	Presented work is aimed to prepare new compounds (O-benzyl-5-chlorosalicyl-tripeptide aldehydes, epoxides, boronic acids and Weinreb amides) which should join to a large group of proteasome inhibitors including bortezomib (Velcade®), ixazomib (MLN-9708, clinical trials: phase I II), delanzomib (CEP-18770, clinical trials: phase I-II), marizomib (clinical trials: phase I), carfilzomib (Kyprolis®). Due to a very similar constitution of mentioned they are expected to bear very similar properties and activities as well. Inhibition of proteasome via blocking its protein recycling function is one of promising ways to treat tumor cells or multiple myeloma. During the synthesis a partial racemization occurred and diasteroisomers were formed. To avoid the racemization, to get exact stereospecific synthesis and defined product are the aims, which are achieved by suitable adjustment of used reagents and their ratios. The details are discussed in the following contribution. Prepared compounds are going to be tested as proteasomal and protein kinase inhibitors, for the type of caused apoptosis and antimicrobial activity.	inhibitor proteasomu