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Preparing and Antiproteasomal Activity of Salycilamides-based Pseudopeptides with Acrylamide Moiety

Authors: Pilařová Eliška | Imramovský Aleš | Pauk Karel | Magar Pratibha | Jorda Radek | Kryštof Vladimír

Year: 2019

Type of publication: ostatní - přednáška nebo poster

Page from-to: nestránkováno

Titles:

Language	Name	Abstract	Keywords
eng	Preparing and Antiproteasomal Activity of Salycilamides-based Pseudopeptides with Acrylamide Moiety	Proteasome is 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.1 We recently developed novel O-benzyl salicylamide-based inhibitors built from leucine and phenylalanine with nanomolar antiproteasomal activity.2 We found a strong correlation between proteasome inhibition and antiproliferative effect in all cell lines assayed. The most potent compounds demonstrated cellular effects corresponding to proteasome inhibition, including dose-dependent accumulation of polyubiquitinylated proteins and induction of apoptosis in multiple myeloma cells.2 To follow our recent studies we synthetized and fully characterized a new series of O-benzyl salicylamides having dipeptide or tripeptide chain containing optically pure leucines or phenylalanines (or a combination) and terminated with acrylamide moiety.3 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.	Antiproteasomal Activity; Salycilamides; Pseudopeptides; Acrylamide