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Pro/antioxidant status of isolated human blood lymphocytes treated with a newly synthesized compound D11-(furan-2-yl)-9-hydroxy-3,11-dihydro-2H-benzo[6,7]thiochromeno[2,3-d]thiazole-2,5,10-trione

О. P. Sen’, О. K. Оnufrovych, M. Ye. Kushynska, О. I. Pershyn,
А. S. Besedina, R. V. Fafula*, Z. D. Vorobets

Danylo Halytsky Lviv National Medical University, Ukraine;
*e-mail: roman_fafula@ukr.net

Received: 20 October 2025; Revised: 23 February 2026;
Accepted: 03 April 2026; Available on-line: April 2026

It is known that 1,4-naphthoquinone derivatives form the basis of a wide range of pharmaceuticals with diverse biological activities. A newly synthesized compound of this group – 11-(furan-2-yl)-9-hydroxy-3,11-dihydro-2H-benzo[6,7]thiochromeno[2,3-d]thiazole-2,5,10-trione, designated by Les-6400 laboratory code, is noteworthy for its drug-like properties. The aim of the study was to determine the parameters of glutathione antioxidant system in isolated human peripheral blood lymphocytes treated with Les-6400. Saponin-permeabilized lymphocytes from the blood samples of healthy male volunteers aged 20–44 years were used in the study. A significant dose-dependent increase in the lipid peroxidation process was observed upon lymphocytes exposure to Les-6400 at concentrations of 10–5–10–3 M. At the concentrations studied no effect of Les-6400 on GSH level was observed, while in the 10–4–10–3 M concentration range the activity of glutathione antioxidant enzymes was markedly affected: the activity of both glutathione peroxidase and glutathione reductase was increased, while that of glutathione-S-transferase was reduced. Thus, Les-6400 had a pronounced effect on the pro/antioxidant status of blood lymphocytes.

Selected 5-amino-1-aryl-1H-1,2,3-triazole scaffolds as promising antiproliferative agents

N. Pokhodylo1*, O. Shyyka1, N. Finiuk2, R. Stoika2

1Ivan Franko National University of Lviv, Ukraine;
2Institute of Cell Biology, National Academy of Sciences of Ukraine, Lviv;
*e-mail: pokhodylo@gmail.com; stoika@cellbiol.lviv.ua

Received: 09 January 2020; Accepted: 25 June 2020

Development of a new effective drugs with low side effects and definite chemical characteristics needs indentification of bioactive scaffolds for further structural optimization. New synthesized derivatives of 4-hetaryl-5-amino-1-aryl-1H-1,2,3-triazoles and 3H-[1,2,3]triazolo[4,5-b]pyridines were tested for anticancer activity using 60 human tumor cell lines within 9 cancer types. The selective influence of (5-amino-1H-1,2,3-triazol-4-yl)quinazolin-4(3H)-ones: 2-(5-amino-1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl)quinazolin-4(3H)-one and 2-(5-amino-1-phenyl-1H-1,2,3-triazol-4-yl)-6-bromoquinazolin-4(3H)-one on ovarian cancer OVCAR-4 cells with growth percentage (GP) = -4.08 and 6.63%, respectively, was found. The derivative  5,7-diamino-3-(3-(trifluoromethyl)phenyl)-3H-[1,2,3]triazolo[4,5-b]pyridine-6-carbonitrile possessed high activity towards lung cancer EKVX cells (GP = 29.14%). The compounds were shown to be less toxic than doxorubicin towards non-tumor human embryonic kidney cells of HEK293 line. Thus, the results of our study confirm the anticancer potential of compounds based on 5-amino-1-aryl-1H-1,2,3-triazoles scaffolds and their fused polycyclic derivatives.