SYNTHESIS AND BIOLOGICAL EVALUATION OF BASIC
AMINOACETOPHENONE-DERIVED KETIMINES

k 2025

SYNTHESIS AND BIOLOGICAL EVALUATION OF BASIC AMINOACETOPHENONE-DERIVED KETIMINES

MURGAŠOVÁ, Veronika; Jovana LISIČIĆ; Ondřej SMIŠTÍK; Jan HOŠEK; Oldřich FARSA et al.

Základní údaje

Originální název

SYNTHESIS AND BIOLOGICAL EVALUATION OF BASIC AMINOACETOPHENONE-DERIVED KETIMINES

Autoři

MURGAŠOVÁ, Veronika ; Jovana LISIČIĆ; Ondřej SMIŠTÍK; Jan HOŠEK a Oldřich FARSA

Vydání

59th Advances in Organic, Bioorganic and Pharmaceutical Chemistry: "Liblice 2025" 2025

Další údaje

Jazyk

angličtina

Typ výsledku

Prezentace na konferencích

Obor

10401 Organic chemistry

Utajení

není předmětem státního či obchodního tajemství

Označené pro přenos do RIV

Ano

Organizační jednotka

Farmaceutická fakulta

Klíčová slova anglicky

schiff bases; basic acetophenone derivative; metalloenzyme inhibitor

Změněno: 5. 1. 2026 15:07, Mgr. Veronika Murgašová

Anotace

V originále

Schiff bases are versatile ligands widely used in metal coordination chemistry, capable of forming stable complexes with a wide variety of metal ions. These metal-ligand 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 play a crucial role in a number of enzymatic reactions. One potential target enzyme is aminopeptidase N (AP-N), a neutral zinc-binding metalloenzyme. Inhibitors of this ubiquitous enzyme may offer effective and broad-spectrum therapeutic applications. Both AP-N and the nuclear factor kappa-B (NF-κB) are critical components involved in various cellular processes, including immune regulation and inflammation. AP-N, which plays a role in peptide metabolism, and NF-κB, a key transcription factor in inflammatory pathways, appear to be functionally connected in the regulation of inflammation and immune response. AP-N may influence NF-κB activation through the metabolism of peptides involved in inflammatory pathways. These two factors may also cooperate in the context of cancer biology and metastasis. The series of basic thiosemicarbazone, semicarbazone, and oxime 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 pro-inflammatory transcription factor NF-κB, in an effort to uncover deeper connections between AP-N inhibition and inflammation-related signaling pathways.

Návaznosti

MUNI/A/1496/2024, interní kód MU

Název: Syntéza a stanovení biologické účinnosti derivátů ketiminů a jejich inhibiční aktivity na metaloenzymy, a též dalších aktivit na pokročilých biologických systémech

Investor: Masarykova univerzita, Syntéza a stanovení biologické účinnosti derivátů ketiminů a jejich inhibiční aktivity na metaloenzymy, a též dalších aktivit na pokročilých biologických systémech

Citovat

MURGAŠOVÁ, Veronika; Jovana LISIČIĆ; Ondřej SMIŠTÍK; Jan HOŠEK a Oldřich FARSA. SYNTHESIS AND BIOLOGICAL EVALUATION OF BASIC AMINOACETOPHENONE-DERIVED KETIMINES. In 59th Advances in Organic, Bioorganic and Pharmaceutical Chemistry: "Liblice 2025". 2025.

@proceedings{2544157,
   author = {Murgašová, Veronika and Lisičić, Jovana and Smištík, Ondřej and Hošek, Jan and Farsa, Oldřich},
   booktitle = {59th Advances in Organic, Bioorganic and Pharmaceutical Chemistry: "Liblice 2025"},
   keywords = {schiff bases; basic acetophenone derivative; metalloenzyme inhibitor},
   language = {eng},
   title = {SYNTHESIS AND BIOLOGICAL EVALUATION OF BASIC AMINOACETOPHENONE-DERIVED KETIMINES},
   year = {2025}
}

TY  - CONF
ID  - 2544157
AU  - Murgašová, Veronika - Lisičić, Jovana - Smištík, Ondřej - Hošek, Jan - Farsa, Oldřich
PY  - 2025
TI  - SYNTHESIS AND BIOLOGICAL EVALUATION OF BASIC AMINOACETOPHENONE-DERIVED KETIMINES
KW  - schiff bases
KW  - basic acetophenone derivative
KW  - metalloenzyme inhibitor
N2  - Schiff bases are versatile ligands widely used in metal coordination chemistry, capable of forming stable complexes with a wide variety of metal ions. These metal-ligand 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 play a crucial role in a number of enzymatic reactions. One potential target enzyme is aminopeptidase N (AP-N), a neutral zinc-binding metalloenzyme. Inhibitors of this ubiquitous enzyme may offer effective and broad-spectrum therapeutic applications. Both AP-N and the nuclear factor kappa-B (NF-κB) are critical components involved in various cellular processes, including immune regulation and inflammation. AP-N, which plays a role in peptide metabolism, and NF-κB, a key transcription factor in inflammatory pathways, appear to be functionally connected in the regulation of inflammation and immune response. AP-N may influence NF-κB activation through the metabolism of peptides involved in inflammatory pathways. These two factors may also cooperate in the context of cancer biology and metastasis. The series of basic thiosemicarbazone, semicarbazone, and oxime 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 pro-inflammatory transcription factor NF-κB, in an effort to uncover deeper connections between AP-N inhibition and inflammation-related signaling pathways.
ER  -

MURGAŠOVÁ, Veronika; Jovana LISIČI$\backslash$'C; Ondřej SMIŠTÍK; Jan HOŠEK a Oldřich FARSA. SYNTHESIS AND BIOLOGICAL EVALUATION OF BASIC AMINOACETOPHENONE-DERIVED KETIMINES. In \textit{59th Advances in Organic, Bioorganic and Pharmaceutical Chemistry: ''Liblice 2025''}. 2025.

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