Synthesis, in silico and investigation of anti-breast cancer activity of new diphenyl urea derivatives: Experimental and computational study

GÖMEÇ, Muhammed; Sayın, Koray; Özkaraca, Mustafa; Özden, Hüseyin

doi:10.1016/j.molstruc.2022.133414

Cited by 5 publications

(4 citation statements)

References 23 publications

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“…Conclusions suggest that HsEF has anticancer effects on both breast tumour cells. And its participation might also account for the variations visible among the two cell lines [9]. After HsEF remedy there have been extensively fewer viable cells in MCF-7 cells.…”

Section: Evaluation Of Antitumoral Effect Of Hibiscus Sabdariffa Extr...mentioning

confidence: 99%

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Remedy on Breast Cancer

Arote

2024

J Clin Med Res.

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The fundamental barrier to powerful remedy for breast maximum cancers is still multidrug resistance due to its severe natural outcomes. The triterpenoid molecule ursolic acid has been considered a capability neoplastic chemo preventive medicine. In numerous preclinical trials an aromatase inhibitor known as letrozole is used to treat Post-Menopausal Women with superior habitual and metastatic breast cancer. The authors may be able to discover a new remedy for the treatment of breast most cancers through identifying the ones who've element consequences much like those of letrozole the maximum aspect results were positioned to be shared through letrozole and the dopaminergic agonist ropinirole in line with research dopaminergic agonist’s purpose apoptosis in Leukaemia, Neuroblastoma, Colon, Ovarian and Breast Cancer Cells. Heart failure, esophageal cancer, lymphedema, bone loss are the side effects observed after treating breast cancer.

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Section: Evaluation Of Antitumoral Effect Of Hibiscus Sabdariffa Extr...mentioning

confidence: 99%

“…Breast cancer in mild of the in silico and in vitro tests. Finished within the scope of our work but in vivo and clinical investigations are required to again up the look at [9].…”

Section: Synthesis In Silico and Investigation Of Anti-breast Cancer ...mentioning

confidence: 99%

Remedy on Breast Cancer

Arote

2024

J Clin Med Res.

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“…The XTT study was performed to assess the cytotoxic activity of shRNA-VEGF and shRNA-VEGF loaded NP on the HeLa and NIH 3T3 cells. DMEM (100 L, 10% FBS) was first used to seed cells in 96-well plates, and the cells were then left to incubate overnight (Han et al, 2015;Gömeç et al, 2022;Keawchaoon and Yoksan 2011;Mohammadi, Hashemi and Hosseini 2015;Purbowatiningrum and Ismiyarto 2017). After that, cells were exposed to shRNA-VEGF and shRNA-VEGF loaded NP at a range of doses (0.25, 0.5, 1, 2, and 5 µg/mL) for 24 hours.…”

Section: Cell Viability Assaymentioning

confidence: 99%

In vitro bioactivity and gene silencing effect of shRNA-VEGF loaded chitosan nanoparticles

Doğan

2022

TFSD

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Purpose: In this study, it is aimed to prepare chitosan nanoparticles containing shRNA-VEGF and evaluate their bioactivity by in vitro cell culture studies and to perform mechanical characterization of nanoparticles. Material and Methods: Ionic chelation method was used to prepare nanoparticles. The XTT assay was used to assess the cytotoxic activity of shRNA-VEGF and shRNA-VEGF loaded NP on the HeLa and NIH 3T3 cells. Results: According to the results IC50 values of shRNA-VEGF and NP including shRNA-VEGF were calculated. IC50 values of shRNA-VEGF and NP including shRNA-VEGF were 0.89±0.010 µg/mL and 0.52±0.004 µg/mL on HeLa cell line. Bax quantities of control, shRNA-VEGF, and shRNA-VEGF loaded NP was measured as 23.70±0.27 ng/mg protein, 34.64±0.36 ng/mg protein, and 39.46±0.54 ng/mg protein, respectively. According to the results, cleaved caspase 3 quantities of control, shRNA-VEGF, and shRNA-VEGF loaded NP was measured as 711.70±4.40 pg/mg protein, 767.23±3.82 pg/mg protein, and 825.32±5.06 pg/mg protein, respectively. Conclusion: shRNA-VEGF and shRNA-VEGF loaded NP significantly reduced HeLa cell reproduction in a concentration-dependent manner while generating no cytotoxicity in NIH 3T3 cells. The expression of pro-apoptotic Bax and cleaved caspase 3 proteins was significantly increased by shRNA-VEGF and shRNA-VEGF loaded NP.

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“…A urea or thiourea structure-containing carboxamide group is also an important functional group in various biomolecules. These ureas or thioureas (Figure 1) exhibit various bioactivities, such as antitobacco mosaic virus activity, 10 mosquiticidal activity, 11 antibreast cancer activity, 12 antioxidant activity, 13 vasodilator activity, 14 anti-inflammatory activity, 15 antimicrobial activity, 16 fungicidal activity, 17 insecticidal activity, 18 and gibberellin-like activity. 19 The Fungicide Resistance Action Committee (2023) lists 24 commercial succinate dehydrogenase inhibitor (SDHI) fungicides.…”

Section: ■ Introductionmentioning

confidence: 99%

Novel Pyrazole Acyl(thio)urea Derivatives Containing a Biphenyl Scaffold as Potential Succinate Dehydrogenase Inhibitors: Design, Synthesis, Fungicidal Activity, and SAR

Sun,

Min,

Sun

et al. 2024

J. Agric. Food Chem.

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As part of a program to discover novel succinate dehydrogenase inhibitor fungicides, a series of new pyrazole acyl(thio)urea compounds containing a diphenyl motif were designed and synthesized. Their structures were confirmed by 1 H NMR, HRMS, and single X-ray crystal diffraction analysis. Most of these compounds possessed excellent activity against 10 fungal plant pathogens at 50 μg mL −1 , especially against Rhizoctonia solani, Alternaria solani, Sclerotinia sclerotiorum, Botrytis cinerea, and Cercospora arachidicola. and N-((4′-chloro-[1,1′-biphenyl]-2-yl)carbamoyl)-1,3-dimethyl-1H-pyrazole-4-carboxamide (9g, EC 50 = 1.31 ± 0.15 μg mL −1 ) exhibited activities against S. sclerotiorum that were better than the commercial fungicide bixafen (EC 50 = 9.15 ± 0.05 μg mL −1 ) and similar to the positive control fluxapyroxad (EC 50 = 0.71 ± 0.11 μg mL −1 ). These compounds were not significantly phytotoxic to monocotyledonous and dicotyledonous plants. Structure−activity relationships (SAR) are discussed by substituent effects/molecular docking, and density functional theory analysis indicated that these compounds are succinate dehydrogenase inhibitors.

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Synthesis, in silico and investigation of anti-breast cancer activity of new diphenyl urea derivatives: Experimental and computational study

Cited by 5 publications

References 23 publications

Remedy on Breast Cancer

Remedy on Breast Cancer

In vitro bioactivity and gene silencing effect of shRNA-VEGF loaded chitosan nanoparticles

Novel Pyrazole Acyl(thio)urea Derivatives Containing a Biphenyl Scaffold as Potential Succinate Dehydrogenase Inhibitors: Design, Synthesis, Fungicidal Activity, and SAR

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