Inhibitory effect of synthetic aromatic heterocycle thiosemicarbazone derivatives on mushroom tyrosinase: Insights from fluorescence, 1 H NMR titration and molecular docking studies

Xie, Juan; Dong, Hanwu; Yu, Yanying; Cao, Shuwen

doi:10.1016/j.foodchem.2015.05.124

Cited by 77 publications

(20 citation statements)

References 36 publications

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“…(E)-2-(Thiophen-2-ylmethylene)hydrazinecarbothioamide ( 13g ): Brown solid with an 89% yield. The spectrum of the substance corresponds to the literature [44].…”

Section: Methodsmentioning

confidence: 99%

New Hydrazinothiazole Derivatives of Usnic Acid as Potent Tdp1 Inhibitors

et al. 2019

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Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is a promising therapeutic target in cancer therapy. Combination chemotherapy using Tdp1 inhibitors as a component can potentially improve therapeutic response to many chemotherapeutic regimes. A new set of usnic acid derivatives with hydrazonothiazole pharmacophore moieties were synthesized and evaluated as Tdp1 inhibitors. Most of these compounds were found to be potent inhibitors with IC50 values in the low nanomolar range. The activity of the compounds was verified by binding experiments and supported by molecular modeling. The ability of the most effective inhibitors, used at non-toxic concentrations, to sensitize tumors to the anticancer drug topotecan was also demonstrated. The order of administration of the inhibitor and topotecan on their synergistic effect was studied, suggesting that prior or simultaneous introduction of the inhibitor with topotecan is the most effective.

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“…(E)-2-(Thiophen-2-ylmethylene)hydrazinecarbothioamide ( 13g ): Brown solid with an 89% yield. The spectrum of the substance corresponds to the literature [44].…”

Section: Methodsmentioning

confidence: 99%

New Hydrazinothiazole Derivatives of Usnic Acid as Potent Tdp1 Inhibitors

et al. 2019

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“…Thiosemicarbazones with aromatic heterocyclic substituents have gained interest of researchers, presenting an alternative for aromatic benzene moiety. Xie et al 40 investigated influence of thiophene, furan and pyrrole rings (Fig. 14) on the inhibition potency of investigated compounds towards tyrosinase.…”

Section: Substitution Of Thiosemicarbazone Scaffold With Alkyl Chain mentioning

confidence: 99%

Thiosemicarbazones with tyrosinase inhibitory activity

Hałdys

Latajka

2019

Med. Chem. Commun.

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“…1 H NMR spectroscopic titration studies of XOD and SA were performed using the previously published method by Xie, Dong, Yu, and Cao (2016), with some modification. Briefly, 500 µl of SA (10 mM) in DMSO-d6 was titrated with increasing concentrations of XOD (0.25, 0.5, and 1 mg/ml).…”

Section: H Nmr Spectroscopic Titration Assaymentioning

confidence: 99%

Antihyperuricemic effect of dietary polyphenol sinapic acid commonly present in various edible food plants

et al. 2019

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The present study was conducted to evaluate the antihyperuricemic effect of sinapic acid (SA). The results showed that SA potently inhibited xanthine oxidase (XOD) in a dose-dependent manner by entering the enzyme active site and thwarting the entrance of the substrate. These results were further confirmed by the quantum chemical descriptors analysis and 1 H NMR titration analysis. The in vivo results indicated that SA not only has the potential to inhibit serum and hepatic XOD (p < .05), but also remarkably lowered serum and urine uric acid levels at 50 and 100 mg/kg bw.Furthermore, SA regulated serum creatinine and blood urea nitrogen levels to normal and lowered inflammation in the renal tubules. Thus, the utilization of SA as an antihyperuricemic agent may have considerable potential for the development of functional foods for the possible treatment of hyperuricemia.

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Inhibitory effect of synthetic aromatic heterocycle thiosemicarbazone derivatives on mushroom tyrosinase: Insights from fluorescence, 1 H NMR titration and molecular docking studies

Cited by 77 publications

References 36 publications

New Hydrazinothiazole Derivatives of Usnic Acid as Potent Tdp1 Inhibitors

New Hydrazinothiazole Derivatives of Usnic Acid as Potent Tdp1 Inhibitors

Thiosemicarbazones with tyrosinase inhibitory activity

Antihyperuricemic effect of dietary polyphenol sinapic acid commonly present in various edible food plants

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