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Novel dipeptide salicylamides, their biological activities, cytotoxicity and proteasomal activity

Authors: Imramovský Aleš | Magar Pratibha | Pauk Karel | Řezníčková Eva | Jorda Radek | Kryštof Vladimír

Year: 2018

Type of publication: ostatní - přednáška nebo poster

Page from-to: nestránkováno

Titles:

Language	Name	Abstract	Keywords
eng	Novel dipeptide salicylamides, their biological activities, cytotoxicity and proteasomal activity	Combination of salicylic moiety, amino acids and basic anilines form specific type of compounds are able to induce apoptosis in cancer cell lines in vitro as well as sensitizes cancer cells to metabolic stress by disrupting actin cytoskeleton and inhibiting autophagic flux. Under base of this results a new salicylamide dipeptides were designed, synthesized and fully characterized. The biological screening of antiproliferative and cytotoxic activities in cancer cell lines in vitro for targeted molecules as well as for chosen intermediates was provided. Biological evaluation shown interesting results for antiproliferative properties. Several intermediates were modified to obtain new compounds with various functional groups. These compounds were tested for their inhibition of protesomal activity. Chosen members shown significant inhibition of proteasome. This group was further extended with novel functional groups, which were tested. Results will be discussed in presented poster.	Dipeptide salicylamides; cytotoxicity; antiproliferative activity; cancer