SYNTHESIS AND EVALUATION OF AMINOACETOPHENONE-DERIVED KETIMINES AS POTENTIAL THERAPEUTIC AGENTS

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216224%3A14160%2F25%3A00143092" target="_blank" >RIV/00216224:14160/25:00143092 - isvavai.cz</a>

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

SYNTHESIS AND EVALUATION OF AMINOACETOPHENONE-DERIVED KETIMINES AS POTENTIAL THERAPEUTIC AGENTS

Popis výsledku v původním jazyce

Schiff bases are versatile ligands widely used in metal coordination chemistry, capable of forming stable complexes with a broad range of metal ions. These complexes exhibit extensive therapeutic potential, including antibacterial, antifungal, antiviral, antimalarial, anti-inflammatory, cytotoxic, enzyme-inhibitory, and anticancer properties. Due to their ability to form such complexes, many Schiff bases also serve as important intermediates in various enzymatic reactions. One potential target enzyme is aminopeptidase N (AP-N), a neutral zinc-binding metalloenzyme. Inhibitors of this ubiquitous enzyme may offer broad-spectrum therapeutic applications. Both AP-N and the nuclear factor kappa-B (NF-κB) are critical components involved in various cellular processes. The series of basic thiosemicarbazone, semicarbazone, and hydroxylamine derivatives of acetophenone with diverse substitution of various symmetrical secondary amines and heterocyclic amines, were synthesized. Compounds showing the most potent inhibitory activity against AP-N (based on IC50 values) were further tested for their ability to inhibit cell proliferation in three different cell lines. These lead compounds are now also being tested for their potential to inhibit the proinflammatory transcription factor NF-κB, in an effort to uncover deeper connections between AP-N inhibition and inflammation-related signaling pathways.

Název v anglickém jazyce

SYNTHESIS AND EVALUATION OF AMINOACETOPHENONE-DERIVED KETIMINES AS POTENTIAL THERAPEUTIC AGENTS

Popis výsledku anglicky

Schiff bases are versatile ligands widely used in metal coordination chemistry, capable of forming stable complexes with a broad range of metal ions. These complexes exhibit extensive therapeutic potential, including antibacterial, antifungal, antiviral, antimalarial, anti-inflammatory, cytotoxic, enzyme-inhibitory, and anticancer properties. Due to their ability to form such complexes, many Schiff bases also serve as important intermediates in various enzymatic reactions. One potential target enzyme is aminopeptidase N (AP-N), a neutral zinc-binding metalloenzyme. Inhibitors of this ubiquitous enzyme may offer broad-spectrum therapeutic applications. Both AP-N and the nuclear factor kappa-B (NF-κB) are critical components involved in various cellular processes. The series of basic thiosemicarbazone, semicarbazone, and hydroxylamine derivatives of acetophenone with diverse substitution of various symmetrical secondary amines and heterocyclic amines, were synthesized. Compounds showing the most potent inhibitory activity against AP-N (based on IC50 values) were further tested for their ability to inhibit cell proliferation in three different cell lines. These lead compounds are now also being tested for their potential to inhibit the proinflammatory transcription factor NF-κB, in an effort to uncover deeper connections between AP-N inhibition and inflammation-related signaling pathways.

Druh

O - Ostatní výsledky

CEP obor

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OECD FORD obor

30104 - Pharmacology and pharmacy

Projekt

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Návaznosti

S - Specificky vyzkum na vysokych skolach

Rok uplatnění

2025

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů