Indole-derived chalcones as anti-dermatophyte agents: In vitro evaluation and in silico study

Mirzaei, Hassan; Abastabar, Mahdi; Emami, Saeed

doi:10.1016/j.compbiolchem.2019.107189

Cited by 8 publications

(3 citation statements)

References 38 publications

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“…10, Table 10, MIC: 1–32 μg mL −1 ) obtained by 4-methoxy base-substitution. 126 Derivative 85 (Fig. 10, Table 10, IC 50 : 3.2 nM) showed significant anti-proliferative activity against HCT-116 cells.…”

Section: Flavonoid-indole Derivativesmentioning

confidence: 99%

Research status of indole-modified natural products

Duan,

Song,

Guo

et al. 2023

RSC Med. Chem.

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Section: Flavonoid-indole Derivativesmentioning

confidence: 99%

Research status of indole-modified natural products

Duan,

Song,

Guo

et al. 2023

RSC Med. Chem.

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“…Mirzaei et al have demonstrated that a series of indole-derived methoxylated chalcones 25 ( Figure 17 ) as anti-dermatophyte agents 64 . Most of the compounds showed strong antifungal activity in the antifungal susceptibility tests of different dermatophytes in vitro .…”

Section: Aromatic Ring Modificationsmentioning

confidence: 99%

A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors

Liu

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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Microtubules play an important role in the process of cell mitosis and can form a spindle in the mitotic prophase of the cell, which can pull chromosomes to the ends of the cell and then divide into two daughter cells to complete the process of mitosis. Tubulin inhibitors suppress cell proliferation by inhibiting microtubule dynamics and disrupting microtubule homeostasis. Thereby inducing a cell cycle arrest at the G2/M phase and interfering with the mitotic process. It has been found that a variety of chalcone derivatives can bind to microtubule proteins and disrupt the dynamic balance of microtubules, inhibit the proliferation of tumour cells, and exert anti-tumour effects. Consequently, a great number of studies have been conducted on chalcone derivatives targeting microtubule proteins. In this review, synthetic or natural chalcone microtubule inhibitors in recent years are described, along with their structure-activity relationship (SAR) for anticancer activity.

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“…Natural and chemical synthetic chalcones have been revealed to play critical roles in some biological functions, such as inflammation [7][8][9] and antibacterial effects [10,11]. Furthermore, more studies demonstrated that chalcones could inhibit tumor progression in various cancers [12][13][14][15][16][17][18][19], including glioma [15,18].…”

Section: Introductionmentioning

confidence: 99%

Chalcone 9X Contributed to Repressing Glioma Cell Growth and Migration and Inducing Cell Apoptosis by Reducing FOXM1 Expression In Vitro and Repressing Tumor Growth In Vivo

Li¹,

Wang²,

Guo³

et al. 2022

BioMed Research International

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Objective. Natural and synthetic chalcones played roles in inflammation and cancers. Chalcone 9X was an aromatic ketone that was found to inhibit cell growth of hepatic cancer and lung cancer cells. In this study, we wanted to investigate the functions of Chalcone 9X in glioma. Materials and Methods. Chemical Chalcone 9X was added in human glioma cell lines (U87 and T98G cells) and normal astrocyte cell lines (HA1800) with various concentrations (0 μmol/L, 20 μmol/L, 50 μmol/L, and 100 μmol/L). CCK-8 assay was used to measure cell viability. Flow cytometric assay was used to measure cell apoptotic rates. Wound healing assay and transwell assay were used to measure cell invasion. RT-PCR was used to detect relative mRNA expressions, and the protein expressions were detected by western blot (WB) and immunohistochemical staining (IHC). Finally, nude mouse xenograft assay was performed to prove the effects of Chalcone 9X in vivo. Results. Results revealed that Chalcone 9X treatment suppressed cell viability and cell migration capacity; it could also induce cell apoptosis in U87 and T98G cells with dose dependence. However, it had little cytotoxicity to normal astrocyte HA1800 cells. Moreover, Chalcone 9X treatment could repress the mRNA and protein expressions of FOXM1 in human glioma cell lines, which was an oncogene that could promote the progression and malignancy of glioma. In addition, FOXM1 overexpression dismissed the Chalcone 9X effects on cell proliferation, apoptosis, and migration in human glioma cell lines. Finally, in vivo assay showed that Chalcone 9X treatment repressed the expression of FOXM1, which inhibited the tumor growth of a xenograft model injected with U87 in nude mice. Conclusions. In all, we found that Chalcone 9X could suppress cell proliferation and migration and induce cell apoptosis in human glioma cells, while it has little cytotoxicity to normal astrocyte cells. Therefore, we uncovered a novel way that Chalcone 9X could inhibit FOXM1 expression and repress the progression and biofunctions of glioma cells, which might be a potential therapeutic drug for treating human glioma.

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Indole-derived chalcones as anti-dermatophyte agents: In vitro evaluation and in silico study

Cited by 8 publications

References 38 publications

Research status of indole-modified natural products

Research status of indole-modified natural products

A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors

Chalcone 9X Contributed to Repressing Glioma Cell Growth and Migration and Inducing Cell Apoptosis by Reducing FOXM1 Expression In Vitro and Repressing Tumor Growth In Vivo

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