Publication detail

Preparation of pseudopeptide aldehydes and vinyl sulfones as a potencional proteasome inhibitors

Authors: Pilařová Eliška | Imramovský Aleš | Pauk Karel | Jorda R | Kryštof V

Year: 2021

Type of publication: ostatní - přednáška nebo poster

Page from-to: nestránkováno

Titles:

Language	Name	Abstract	Keywords
eng	Preparation of pseudopeptide aldehydes and vinyl sulfones as a potencional proteasome inhibitors	Proteasome is 2,5 MDa large multi-subunit complex responsible for the protein degradation in cells. Inhibition of this process is one of strategies for suppression of uncontrolled proliferation of multiple myeloma or leukemia cancer cell lines.We developed novel O-benzyl salicylamide-based inhibitors built from leucine and phenylalanine with nanomolar antiproteasomal activity. To follow our studies we synthetized and fully characterized a new series of O-benzylsalicylamides having tripeptide chain containing optically pure aminoacids (L-Leu, L-Trp, L-NLeu, L-CHA, L-Pro, L-Phe) and terminated with aldehyde or vinyl sulfone warhead. All novel salicylamides were tested for their antiproliferative properties against various cancer cell lines derived from hematopoietic malignancies and the resulting data will be presented.	pseudopeptide aldehydes; pseudopeptide vinyl sulfones; proteasome inhibitors

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