Aromatic sulphonamides of aziridine-2-carboxylic acid derivatives as novel PDIA1 and PDIA3 inhibitors

In this study, we report a series of newly synthesised sulphonamides of aziridine-2-carboxylic acid (Az-COOH) ester and amide analogues as potent protein disulphide isomerase (PDI, EC 5.3.4.1) inhibitors. The inhibitory activity on PDI was determined against recombinant human PDIA1 and PDIA3 protein...

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Veröffentlicht in:	Journal of enzyme inhibition and medicinal chemistry 2023-12, Vol.38 (1), p.2158187-2158187
Hauptverfasser:	Zelencova-Gopejenko, D., Andrianov, V., Domracheva, I., Kanepe-Lapsa, I., Milczarek, M., Stojak, M., Przyborowski, K., Fedak, F. A., Walczak, M., Kramkowski, K., Wietrzyk, J., Chlopicki, S., Kalvins, I.
Format:	Artikel
Sprache:	eng
Schlagworte:	Acids aziridine Aziridines - pharmacology Cancer Carboxylic acids Chemistry Disulphide Enzymes Humans inhibitor isomerase Ligands NMR Nuclear magnetic resonance PDI Protein Disulfide-Isomerases - antagonists & inhibitors Protein Disulfide-Isomerases - chemistry Proteins Research Paper Spectroscopy Sulfonamides Sulfonamides - pharmacology
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