The Synthesis, Characterization, and Anticancer Activity of New 2-acetylbenzofuran-Chalcone Hybrids

Coskun, Demet; Dalkılıç, Semih; Dalkılıç, Lütfiye Kadıoğlu; Çoşkun, Mehmet

doi:10.1007/s40995-021-01166-5

Cited by 9 publications

(7 citation statements)

References 39 publications

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“…No shift or a one-step shift may point out a bactericidal mode of action. The bactericidal mode of action was recognized in some natural chalcones, such as xanthohumol and chalcone-based derivatives ( Ahmed et al, 2019 ; Bocquet et al, 2019 ; Xu et al, 2019 ; Coskun et al, 2021 ). Among halogenated chalcone derivatives, the bactericidal action against SA, or MRSA has been explored in fluorinated chalcone-1,2,3-triazole hybrids, or chlorinated benzofuran chalcones ( Xu et al, 2019 ; Coskun et al, 2021 ).…”

Section: Resultsmentioning

confidence: 99%

Comprehensive insight into anti-staphylococcal and anti-enterococcal action of brominated and chlorinated pyrazine-based chalcones

Konečná

Diepoltová²,

Holmanová³

et al. 2022

Front. Microbiol.

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The greatest threat and medicinal impact within gram-positive pathogens are posed by two bacterial genera, Staphylococcus and Enterococcus. Chalcones have a wide range of biological activities and are recognized as effective templates in medicinal chemistry. This study provides comprehensive insight into the anti-staphylococcal and anti-enterococcal activities of two recently published brominated and chlorinated pyrazine-based chalcones, CH-0y and CH-0w. Their effects against 4 reference and 12 staphylococcal and enterococcal clinical isolates were evaluated. Bactericidal action, the activity in combination with selected conventional antibiotics, the study of post-antimicrobial effect (PAE, PAE/SME), and in vitro and in vivo toxicity, were included. In CH-0y, anti-staphylococcal activity ranging from MIC = 15.625 to 62.5 μM, and activity against E. faecium from 31.25 to 62.5 μM was determined. In CH-0w, anti-staphylococcal activity ranging from 31.25 to 125 μM, and activity against E. faecium and E. faecalis (62.5 μM) was revealed. Both CH-0y and CH-0w showed bactericidal action, beneficial impact on bacterial growth delay within PAE and PAE/SME studies, and non/low toxicity in vivo. Compared to CH-0w, CH-0y seems to have higher anti-staphylococcal and less toxic potential. In conclusion, chalcones CH-0y and CH-0w could be considered as structural pattern for future adjuvants to selected antibiotic drugs.

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Section: Resultsmentioning

confidence: 99%

Comprehensive insight into anti-staphylococcal and anti-enterococcal action of brominated and chlorinated pyrazine-based chalcones

Konečná

Diepoltová²,

Holmanová³

et al. 2022

Front. Microbiol.

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“…[63] Further studies indicated that incorporation of furan or thiophene fragment was permitted, and hybrids 42a,b (IC 50 : 1.248 and 0.871 µM, MTT assay) exhibited potent antiproliferative activity against MDA-MB-231 cancer cells. [64] Chalcone-furan hybrids 43a,b not only showed considerable antiproliferative activity (IC 50 : 9.41 and 10.76 µM, MTT assay) against MCF-7 cancer cells, but also were nontoxic (IC 50 : >50 µM) toward normal 3T3 cells. [65] Mechanistically, hybrid 43a activated and MDA-MB-231 breast cancer cell lines.…”

Section: Chalcone-furan/thiophene Hybridsmentioning

confidence: 98%

Section: Chalcone‐furan/thiophene Hybridsmentioning

confidence: 99%

Current scenario of chalcone hybrids with antibreast cancer therapeutic applications

Wang,

Zhu,

Zhang

et al. 2024

Archiv der Pharmazie

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Breast cancer, an epithelial malignant tumor that occurs in the terminal ducts of the breast, is the most common female malignancy. Currently, approximately 70%–80% of breast cancer with early‐stage, nonmetastatic disorder is curable, but the emergency of drug resistance often leads to treatment failure. Moreover, advanced breast cancer with distant organ metastases is incurable with the available therapeutics, creating an urgent demand to explore novel antibreast cancer agents. Chalcones, the precursors for flavonoids and isoflavonoids, exhibit promising activity against various breast cancer hallmarks, inclusive of proliferation, angiogenesis, invasion, metastasis, inflammation, stemness, and regulation of cancer epigenetics, representing useful scaffolds for the discovery of novel antibreast cancer chemotherapeutic candidates. In particular, chalcone hybrids could act on two or more different biological targets simultaneously with more efficacy, lower toxicity, and less susceptibility to resistance. Accordingly, there is a huge scope for application of chalcone hybrids to tackle the present difficulties in breast cancer therapy. This review outlines the chalcone hybrids with antibreast cancer potential developed from 2018. The structure–activity relationships as well as mechanisms of action are also discussed to shed light on the development of more effective and multitargeted chalcone candidates.

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“…By reading the control wells, the absorbance values obtained were averaged and this value was accepted as 100% live cell. The absorbance values obtained from the wells of plant extract were compared to the control absorbance value and percent viability values were calculated (Coskun et al, 2021;Dalkilic et al, 2021). The absorbance values measured with the plate reader device were recorded, then the measured absorbance values were compared with the control groups.…”

Section: Mtt Assay Applicationmentioning

confidence: 99%

Investigation of apoptotic, cytotoxic, and antioxidant effects of Juglans regia against MDA-MB-231 and A549 cell lines

Dalkılıç

Uygur

2023

ijpbp

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Cancer is one of the most common pathologies in the world, which for centuries has led to a decline in the standard of living and even death of many people. In short, cancer is a disease that occurs when mutations in genes that limit and regulate cell proliferation, survival, and movement are reflected in somatic cells. In recent years, there have been many new and promising developments in the world of science for cancer treatment. However, due to the side effects of some treatments, the cost of others, and the fact that some drugs are still in the trial phase, it has not yet reached the expected level of treatment and success. This has encouraged the scientific community to investigate natural agents due to their lower cost and limited side effects. Juglans regia L., popularly known as walnut, is a plant containing many natural compounds that have been used both as a foodstuff and for various medicinal purposes from past to present. As a result of the literature review, it is known that walnut has many medicinal and biological properties, especially antiinflammatory, antifungal and antiallergic properties. In this study, the outer shells of J. regia were used and the components of these shells were extracted with three different solvents: methanol, ethanol, and hexane. These extracts were used in cytotoxic activity and antioxidant activity assays. The antioxidant activity of the extract was determined using a DPPH assay. Cytotoxic activity was determined by MTT assay using a breast cancer cell line (MDA-MB-231). J. regia extracts were found to have significant cytotoxic activity on the MDA-MB-231 cell line. It has been observed that the outer bark of J. regia showed more potent anticancer effects than antioxidant activity. According to the results obtained from the study, the antioxidant and cytotoxic effect of the outer bark of J. regia is thought to contribute significantly to the identification of new active substances for cancer treatment. Therefore, further studies are needed to fully determine the effects of the outer bark of J. regia.

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The Synthesis, Characterization, and Anticancer Activity of New 2-acetylbenzofuran-Chalcone Hybrids

Cited by 9 publications

References 39 publications

Comprehensive insight into anti-staphylococcal and anti-enterococcal action of brominated and chlorinated pyrazine-based chalcones

Comprehensive insight into anti-staphylococcal and anti-enterococcal action of brominated and chlorinated pyrazine-based chalcones

Current scenario of chalcone hybrids with antibreast cancer therapeutic applications

Investigation of apoptotic, cytotoxic, and antioxidant effects of Juglans regia against MDA-MB-231 and A549 cell lines

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