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Publikace detail

Synthesis of salicylamide-based pseudopeptides terminated with aldehydes or vinyl sulfone functional group as potential proteasome inhibitors
Autoři: Pilařová Eliška | Imramovský Aleš | Pauk Karel | Magar Pratibha | Jorda Radek | Kryštof Vladimír
Rok: 2019
Druh publikace: ostatní - přednáška nebo poster
Strana od-do: nestránkováno
Tituly:
Jazyk Název Abstrakt Klíčová slova
eng Synthesis of salicylamide-based pseudopeptides terminated with aldehydes or vinyl sulfone functional group as potential proteasome inhibitors Our research group developer novel O-benzyl salicylamide-based proteasome inhibitors built from L-leucine and L-phenylalanine.1 These compounds contain various functional groups such as aldehydes or weinreb amides or epoxyketones at the C-end of molecule. Our ongoing research investigated other functional groups with higher stability than aldehyde group. We also investigated influence of amino acid sequence in peptide chain on the inhibition activity. Synthesis of intermediates and targeted molecules was done in respect of high optical purity. Classical approaches known from peptide chemistry were applied and carefully optimized. Several new compounds with aldehyde or vinylsulfone group were prepared (Fig. 1) and their cytotoxicity as well as proteasome inhibition is under evaluation. Proteasome Inhibition; Pseudopeptides; O-benzyl salicylamides