2020
DOI: 10.1007/s00210-020-02025-7
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Induction of Cyp450 enzymes by 4-thiazolidinone-based derivatives in 3T3-L1 cells in vitro

Abstract: Abstract4-Thiazolidinones and related derivatives are regarded as privileged structures in medicinal chemistry and a source of new drug-like compounds. To date it is known that thiazolidinones are able to induce CYP1A1 activity in 3T3-L1 cells. Therefore, to extend the knowledge of the mechanism of thiazolidinones in the cell, four chemically synthesized heterocycles were tested on 3T3-L1 cells. The 3T3-L1 cells were exposed to Les-2194, Les-3640, Les-5935, and Les-6166. Our study showed that 1 μM βNF, Les-219… Show more

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Cited by 5 publications
(12 citation statements)
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References 60 publications
(82 reference statements)
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“…The results have shown that, generally, Les-5935 does not affect negatively the BJ cell line, in contrast to Les-3166, Les-6166, and Les-6009, which are able to significantly decrease the metabolic activity in BJ. Similar results were obtained by Szychowski et al, who proved that Les-5935, even after 72 h treatment, did not show cytotoxicity against mouse fibroblasts [ 28 ]. However, Les-6166 decreased the metabolic activity in the 3T3-L1 mouse cell line after 48 h treatment in a concentration range of 10–100 µM [ 28 ].…”
Section: Discussionsupporting
confidence: 88%
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“…The results have shown that, generally, Les-5935 does not affect negatively the BJ cell line, in contrast to Les-3166, Les-6166, and Les-6009, which are able to significantly decrease the metabolic activity in BJ. Similar results were obtained by Szychowski et al, who proved that Les-5935, even after 72 h treatment, did not show cytotoxicity against mouse fibroblasts [ 28 ]. However, Les-6166 decreased the metabolic activity in the 3T3-L1 mouse cell line after 48 h treatment in a concentration range of 10–100 µM [ 28 ].…”
Section: Discussionsupporting
confidence: 88%
“…One of the classes of heterocycles with promising anticancer activity is the series of 4-thiazolidinone (4-TZD) derivatives. To date, it has been described that various 4-thiazolidinones exhibit anticancer properties demonstrated in numerous in vitro and in vivo models [ 10 , 12 , 13 , 14 , 18 , 25 , 26 , 27 , 28 ]. The determination of the impact of xenobiotics on metabolic activity is one of the most relevant analyses allowing the formulation of preliminary assumptions about their application potential.…”
Section: Discussionmentioning
confidence: 99%
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