Univerzita PardubiceFakulta chemicko- technologická

Univerzita Pardubice

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Publikace detail

Novel potential proteasome inhibitor based on tripeptide scaffold

Autoři: Dušek Jan | Imramovský Aleš

Rok: 2014

Druh publikace: ostatní - přednáška nebo poster

Strana od-do: nestránkováno

Tituly:

Jazyk	Název	Abstrakt	Klíčová slova
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