5-Ene-4-thiazolidinones induce apoptosis in mammalian leukemia cells

Senkiv, Julia; Finiuk, Nataliya; Kaminskyy, Danylo; Havrylyuk, Dmytro; Wojtyra, Magdalena; Kril, Iryna; Gzella, Andrzej; Stoika, Rostyslav; Lesyk, Roman

doi:10.1016/j.ejmech.2016.03.089

Cited by 69 publications

(62 citation statements)

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“…For estimating the impact of ROS’s scavengers (N-acetyl-cysteine (NAC) and ascorbic acid (AA) (Sigma-Aldrich, St. Louis, USA)) on the cytotoxicity of Les-3833 and Dox on WM793 cells were used in a combination with cell pre-treatment for 30 min with the non-toxic concentrations of ROS scavengers (NAC was used in 1.0; 2.0 mM: AA - at 25.0; 100.0 μM) (14). …”

Section: Methodsmentioning

confidence: 99%

“…It was reported that products of the hybridization of thiazolidine-2,4-diones scaffolds with different bioactive molecules possessed anticancer activity (5). It was shown that novel 5-ene-4-thiazolidinones possessed a selective anti-leukemic action (14). A search for novel potent antitumor pharmaceuticals demonstrating high selectivity and low toxicity to normal cells is currently strongly prioritized (5,8,12-14).…”

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confidence: 99%

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4-Thiazolidinone derivative Les-3833 effectively inhibits viability of human melanoma cells through activating apoptotic mechanisms

et al. 2017

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AimTo evaluate cytotoxic action of 4-thiazolidinone derivative Les-3833 and study the mechanisms of its pro-apoptotic action toward human melanoma cells and human tumor cell lines of other tissue origin.MethodsThe effect of Les-3833 or doxorubicin on the viability of 9 cell lines was studied using MTT assay, while human melanoma cells of WM793 line were additionally examined using light and fluorescent microscopies for evaluating cytomorphological changes. The Western-blot and flow cytometric analyses were carried out to study signaling pathways of melanoma cell cycling and death.ResultsLes-3833 was the most efficient against melanoma cells. Its half maximal inhibitory concentration (IC50) was 0.22 μg/mL for WM793 cells and 0.3 μg/mL for SK-Mel-28 melanoma cells. For human lung A549, breast MCF-7, colon HCT116, and ovarian SKOV3 carcinoma cell lines IC50 was in between 2.5 to >5.0 μg/mL. Les-3833 was relatively not toxic (IC50 ˃ 5 μg/mL) for human embryonic kidney HEK293 cells. Results of Annexin V/PI staining of melanoma cells and activation of caspase 3, PARP, MAPK, and EndoG protein suggest apoptosis in Les-3833-treated cells. Les-3833 also induced ROS production in melanoma cells and their arrest in G0/G1 phase of cell cycle.ConclusionNovel 4-thiazolidinone derivative Les-3833 is effective against human melanoma cells in vitro, and such effect is tumor specific since it is much less pronounced in human carcinoma and leukemia cells. In melanoma cells Les-3833 induces apoptosis (morphological changes and increased pro-apoptotic proteins), ROS production, and arrest in G0/G1 phase of cell cycle.

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Section: Methodsmentioning

confidence: 99%

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confidence: 99%

4-Thiazolidinone derivative Les-3833 effectively inhibits viability of human melanoma cells through activating apoptotic mechanisms

et al. 2017

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“…Synthesis and physicochemical data of the compounds used in this study were described previously: Les3882 and Les3288 [19], Les4368 and Les4370 [20,21].…”

Section: Methodsmentioning

confidence: 99%

4-Thiazolidinone-based derivatives rescue TNAα-inhibited osteoblast differentiation in mouse mesenchymal precursor cells

Malysheva¹,

Finiuk²,

Pavlenko³

et al. 2017

Ukr.Biochem.J.

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Rheumatoid arthritis (RA) is an autoimmune inflammatory disease of yet unknown etiology. Tumor necrosis factor α (TNFα are central players in the inhibition of activity of skeletogenesis. The aim of this study was to evaluate the anti-inflammatory activity of novel 4-thiazolidinone-based derivatives towards TNFα-induced pro-inflammatory effects during bone formation. We performed in vitro evaluation of functional effects of 4-thiazolidinones denoted as 0.1, 0.3 and 1.0 μM) on the TNFα-mediated inhibition of the BMP-induced osteoblast differentiation in mouse mesenchymal precursor (stem) cells of C2C12 line. Treatment of these cells with TNFα completely inhibited their myogenic differentiation, as well as strongly inhibited the BMP-induced osteogenesis. Strikingly, the treatment of C2C12 cells with

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“…), 7.67 д (2Н, J = 8.4 Гц , аром. ), 7.59 т (1H, J = 6.7 Гц, піри-дин), 7.62 д (1H, J =7.6 Гц, піридин), 7.98 с (1H, CH), 8.08 т (1H, J = 7.4 Гц, піридин), 8.67 д (1H, J = 5.0 Гц, піридин). 1 H ЯМР спектры снимались на приборе Varian Gemini 400 MHz.…”

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Синтез 3-Піридилзаміщених 4-Тіазолідинонів Як Потенційних Біологічно Активних Сполук

Wojtyra¹,

Lesyk²

2017

ФЧ

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Мета роботи. Здійснити синтез 3-піридилзаміщених 5-ариліден-4-тіазолідинонів потенційних біологічно активних сполук.Матеріали і методи. Вихідні реагенти синтезовані за відомими методиками із комерційно доступних реактивів. 1H ЯМР спектри знімались на приладі Varian Gemini 400 MHz. Температури плавлення визначали на приладі BŰCHI B-545.Результати й обговорення. Одержано 3-піридилзаміщені 5-ариліден-2-тіоксо-4-тіазолідинони на основі методу Гольмберга та реакції Кньовенагеля. Для синтезу структурно подібних 3-(2-піридил)-2,4-тіазолідиндіонів запропоновано двохетапний підхід, який базується на однореакторній («one-pot») трикомпонентній реакції 1-бензоїл-3-(піридин-2-іл)-2-тіосечовини, монохлороцтової кислоти та ароматичного альдегіду з утворенням 5-ариліден-2-бензоїліміно-3-(2-піридил)-4-тіазолідинонів, які при кислотному гідролізі з високими виходами утворюють цільові продукти. Структура синтезованих сполук підтверджена методом спектроскопії ПМР.Висновки. Синтезовано серію нових 3-піридилзаміщених похідних роданіну, тіазолідиндіону і псевдотіогідантоїну. Стереоселективність реакції Кньовенагеля і утворення 5-(Z)-ариліден-4-тіазолідинонів підтверждено даними спектрів ПМР.

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5-Ene-4-thiazolidinones induce apoptosis in mammalian leukemia cells

Cited by 69 publications

References 74 publications

4-Thiazolidinone derivative Les-3833 effectively inhibits viability of human melanoma cells through activating apoptotic mechanisms

4-Thiazolidinone derivative Les-3833 effectively inhibits viability of human melanoma cells through activating apoptotic mechanisms

4-Thiazolidinone-based derivatives rescue TNAα-inhibited osteoblast differentiation in mouse mesenchymal precursor cells

Синтез 3-Піридилзаміщених 4-Тіазолідинонів Як Потенційних Біологічно Активних Сполук

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