Comparative study of the cytotoxic properties of isatin-containing derivatives of 4-thiazolidinone with different structure toward human tumor cells in vitro

Chumak, Vira; Panchuk, R. R.; Manko, Nazar; Havrylyuk, Dmytro; Lesyk, Roman; Kobylinska, Lesya; Zimenkovsky, Borys; Stoika, Rostyslav

doi:10.30970/sbi.0802.357

Cited by 5 publications

(8 citation statements)

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“…Within 20 days of the experiment, we did not observe changes in the appearance, skin condition, behavior, appetite and body weight of the experimental rats of [3][4][5][6][7][8][9] th groups compared to the control group. Only in the second group of animals treated with doxorubicin, a significant reduction in body weight, changes in skin, general weakness and low activity were noticed.…”

Section: Resultsmentioning

confidence: 99%

“…According to the results of our previous studies [8,9], this compound was characterized by the most pronounced cytotoxic effect and possessed the highest toxic effect in rats compared to the effect of other 4-thiazolidinone derivatives. As expected, the drug 3833 demonstrated the highest nephrotoxicity among the 4-thiazolidinone derivatives used in this study.…”

Section: Resultsmentioning

confidence: 99%

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Biochemical indicators of nephrotoxicity in blood serum of rats treated with novel 4-thiazolidinone derivatives or their complexes with polyethylene glycol-containing nanoscale polymeric carrier

nska¹,

Havrylyuk²,

Mitina³

et al. 2016

Ukr.Biochem.J.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Biochemical indicators of nephrotoxicity in blood serum of rats treated with novel 4-thiazolidinone derivatives or their complexes with polyethylene glycol-containing nanoscale polymeric carrier

nska¹,

Havrylyuk²,

Mitina³

et al. 2016

Ukr.Biochem.J.

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“…The compounds of this class are known for their anticancer activity as well as for their other biological effects, such as antibacterial, fungicidal, antiviral, anti-inflammatory, and antidiabetic actions [10]. The results of our previous studies on antitumor efficiency of 4-thiazolidinone derivatives, including those of pyrazoline substitution [9,10] allowed drawing a conclusion that the pyrazoline-thiazolidinone-indoline conjugates demonstrate the most promising results, and that the most active ones are the compounds 3288, 3833 and 3882 [11,12]. The molar masses of these synthetic substances are 559.44 g/ mol (3288), 530.61 g/mol (3882), and 609.51 g/mol (3833).…”

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confidence: 99%

“…In previous studies, we have demonstrated that combining of thiazolidinone, pyrazoline and 2-oxoindoline moieties in a more 'rigid' tricyclic system -3-[2-(3,5-diaryl-4,5-dihydropyrazol-1-yl)-4-oxo-4H-thiazol-5-iliden]-1,3-dihydroindol-2-one -allows us to achieve high cytostatic activity in 60 strains of human cancer cells without a pronounced selective effect [9,12]. All the three compounds -3288, 3833 and 3882 -are structurally similar and belong to a group of pyrazoline-thiazolidinoneisatins which were patented by us and have a noticeable antineoplastic activity in vitro that led us to study their effect on laboratory animals [12,13].…”

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confidence: 99%

Biochemical indicators of hepatotoxicity in blood serum of rats under the effect

Kobylinska¹

2015

Ukr.Biochem.J.

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іnstitute of cell biology, national academy of sciences of ukraine, Lviv the aim of this study was to compare the effect of new synthetic 4-tiazolidinone derivatives (compounds 3882, 3288 and 3833) and doxorubicin (positive control) in free form and in their complexes with synthetic polyethyleneglycol-containing nanoscale polymeric carrier on the biochemical indicators of hepatotoxicity in blood serum of rats. the activity of enzymes considered as the markers of hepatotoxicity, as well as the concentration of total protein, urea and creatinine were measured in blood serum of rats. It was found that after injection of investigated compounds the activities of alanine aminotransferase, alkaline phosphatase and α-amylase increased in comparison to control. Doxorubicin injection was accompanied by 4-fold increase in the activity of γ-glutamyltransferase, and injection of compound 3833 led to 2.5-fold elevation of the activity of this enzyme. complexation of these аntineoplastic derivatives with a synthetic nanocarrier lowered the activity of the investigated enzymes substantially if compared to the effect of these compounds in free form. the most evident decrease was measured for α-amylase, γ-glutamyltransferase and lactate dehydrogenase activities. the normalization of concentrations of total protein, urea and creatinine in blood serum of rats treated with complexes of the studied compounds with a polymeric carrier comparing with their introduction in free form was also detected. thus, the immobilization by novel polymeric carrier of anticancer drugs possessing high general toxicity in the treated organism mitigates their toxic effect, which is evident as normalization of specific biochemical indicators of the hepatodestructive effects of the anticancer drugs.

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“…Les-3833 was highly active towards the non-small-cell lung cancer cell line HOP-92 (GI 50 < 0.01 µM), colon cancer line HCT-116 (GI 50 = 0.018 µM), CNS cancer cell line SNB-75 (GI 50 = 0.0159 µM), ovarian cancer cell line OVCAR-3 (GI 50 = 0.0216 µM), and renal cancer cell line RXF 393 (GI 50 = 0.0197 µM) [18,21]. Les-3833 also demonstrated lower general toxicity in vivo compared with that of doxorubicin [10,[21][22][23][24].…”

Section: Discussionmentioning

confidence: 99%

Biodistribution and Anticancer Characteristics of Les-3833, A Novel 4-thiazolidinone-Based Lead Compound

et al. 2020

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Recently, we identified the promising anticancer potential of the synthetic 4-thiazolidinone-based anticancer lead compound Les-3833 which demonstrated tumor-suppressing action in vitro and in vivo. Based on the results of previous studies, the aim of this research was to investigate the cytotoxicity in vitro and the biodistribution in laboratory mice to support the biotherapeutic drug development of Les-3833. Les-3833 (2.5 mg/kg) was intravenously injected into male Balb/c mice. Measurements were performed at 5 min, 15 min, 1 h, 4 h, and 24 h time points in blood plasma, brain, liver, and kidney using high-performance liquid chromatography/tandem mass spectrometry. After the administration of Les-3833, the maximum level of this compound was observed in plasma at 2.08 min. In the brain, the mean maximum concentration of Les-3833 was 7.17 ng/mL at 5 min, while after 15 min, it was not found. In the liver, at 5 min, the maximum concentration was 1190 ng/g. At 15 min, concentration of Les-3833 in the liver decreased by 14.3%; at 6 h by 22.8%; and after 24 h by 64.7%. Its maximum concentration in kidney was 404 ng/g within 5–15 min, at 1 h it decreased by 36.1%, and after 24 h by 49.3%. Thus, Les-3833 was rapidly taken up by different organs from the bloodstream, partially metabolized in the liver, and excreted mainly through the kidneys, while in the brain, a very low concentration could be observed for only a short period of time.

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Comparative study of the cytotoxic properties of isatin-containing derivatives of 4-thiazolidinone with different structure toward human tumor cells in vitro

Cited by 5 publications

References 9 publications

Biochemical indicators of nephrotoxicity in blood serum of rats treated with novel 4-thiazolidinone derivatives or their complexes with polyethylene glycol-containing nanoscale polymeric carrier

Biochemical indicators of nephrotoxicity in blood serum of rats treated with novel 4-thiazolidinone derivatives or their complexes with polyethylene glycol-containing nanoscale polymeric carrier

Biochemical indicators of hepatotoxicity in blood serum of rats under the effect

Biodistribution and Anticancer Characteristics of Les-3833, A Novel 4-thiazolidinone-Based Lead Compound

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