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Development of New Salicylamide Derivates with Significant Cytotoxicity
Autoři: Magar Pratibha | Jorda Radek | Kryštof Vladimír | Hendrychová Denisa | Imramovský Aleš
Rok: 2019
Druh publikace: ostatní - přednáška nebo poster
Strana od-do: nestránkováno
Tituly:
Jazyk Název Abstrakt Klíčová slova
eng Development of New Salicylamide Derivates with Significant Cytotoxicity In drug discovery, several beneficial properties have been attributed to substituted salicylamide derivatives, mostly investigated for their therapeutic activities such as antimicrobial,1 antifungal,2 or antimitotic and antiplaque agent.3 Previously in our group successfully introduced substituted 2-hydroxy-N-(arylalkyl)-benzamides and salicylamides terminated with aliphatic chains possess interesting antiproliferative properties.4,5 In this study, we designed and synthesized novel salicylamides bearing the combination of optically pure amino acids such as L-phenylalanine or L-leucine which were subsequently tested against K562, CEM, THP-1, G361, MCF-7, HCT-116 cell lines. All 32 novel triamide derivatives show antiproliferative activity in tested cancer cell lines and eight of them reach up single-digits micromolar GI50 (In Fig.1 see general structure of investigated compounds). Salicylamides; Cytotoxicity; Triamide Derivatives; Antiproliferative Activity