2021
DOI: 10.3390/ph14111079
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Effect of Selected Silyl Groups on the Anticancer Activity of 3,4-Dibromo-5-Hydroxy-Furan-2(5H)-One Derivatives

Abstract: The pharmacological effects of carbon to silicon bioisosteric replacements have been widely explored in drug design and medicinal chemistry. Here, we present a systematic investigation of the impact of different silyl groups on the anticancer activity of mucobromic acid (MBA) bearing furan-2(5H)-one core. We describe a comprehensive characterization of obtained compounds with respect to their anticancer potency and selectivity towards cancer cells. All four novel compounds exert stronger antiproliferative acti… Show more

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Cited by 12 publications
(11 citation statements)
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“…These compounds have been shown to exhibit cytotoxic effects [9] and increase the sensitivity of tumor cells to oncogenic viruses [22]. Additionally, as we have shown in our previous work [19], the introduction of a silyl group into the structure of 3,4-dihalogeno-furan-2(5H)-one increases the cytotoxicity of the tested compound with reference to the initial structure. Carbohydrates and their glycoconjugates are involved in many biological processes and play an important role in various diseases.…”
Section: Introductionmentioning
confidence: 76%
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“…These compounds have been shown to exhibit cytotoxic effects [9] and increase the sensitivity of tumor cells to oncogenic viruses [22]. Additionally, as we have shown in our previous work [19], the introduction of a silyl group into the structure of 3,4-dihalogeno-furan-2(5H)-one increases the cytotoxicity of the tested compound with reference to the initial structure. Carbohydrates and their glycoconjugates are involved in many biological processes and play an important role in various diseases.…”
Section: Introductionmentioning
confidence: 76%
“…The furanone scaffold is found in many complex natural products and exhibits diverse biological properties, such as antibacterial [1][2][3][4], anticancer [5][6][7][8][9][10], antifungal [11,12], antiviral [13], anti-inflammatory [14][15][16][17] and antioxidant [15][16][17][18] (Figure 1). In recent years, several derivatives, such as 3,4-dihalogeno-furan-2(5H)-one derivatives, have been obtained, which exhibited various anticancer activities [19,20]. Molecular targets for these derivatives were such key enzymes as kinases, COX-1, topoisomerase I or MDM2-p53 interaction.…”
Section: Introductionmentioning
confidence: 99%
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“…Silyl ether derivatives of tetrahydropyrans (Carrillo et al, 2006, 2007) and of mucobromic acid (Kitel et al, 2021), evaluated for their anticancer activity.…”
Section: Carbon‐silicon Bioisosteric Replacement In Anticancer Drugs ...mentioning
confidence: 99%
“…Walczak and coworkers synthesized a series of silyl ether derivatives of mucobromic acid (MBA) bearing furan‐2(5H)‐one core and evaluated them against a panel of human cancer cell lines (HCT116, HCT‐116 −/− p53, HT‐29, MCF‐7, SJSA‐1, U2OS, HepG2, and Hep3B) using the MTT assay (Kitel et al, 2021). All the silyloxy derivatives exhibited stronger antiproliferative activity than the parent compound, with compounds 59 and 60 (shown in Figure 14) exhibiting noticeable antiproliferative activity primarily on the HCT‐116 cell line (IC 50 = 1.3 and 1.6 μM, respectively), while 61 and 62 appeared to be effective across all tested cancer cells, with IC 50 ranging from 7.3 to 21.3 μM and 3.9 to 65.6 μM, respectively (Kitel et al, 2021). Compound 60 displayed a superior anticancer activity on HCT‐116 and HCT‐116 −/− p35 cell lines but was significantly less active on MCF‐7.…”
Section: Carbon‐silicon Bioisosteric Replacement In Anticancer Drugs ...mentioning
confidence: 99%