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

Result code in 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>

Result on the web

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DOI - Digital Object Identifier

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Result language

angličtina

Original language name

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

Original language description

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.

Czech name

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Czech description

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Type

O - Miscellaneous

CEP classification

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OECD FORD branch

30104 - Pharmacology and pharmacy

Project

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Continuities

S - Specificky vyzkum na vysokych skolach

Publication year

2025

Confidentiality

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