Novel benzimidazole derivatives: Synthesis, in vitro cytotoxicity, apoptosis and cell cycle studies

Atmaca, Harika; İlhan, Süleyman; Batır, Muhammet Burak; Pulat, Çisil Çamlı; Güner, Adem; Bektaş, Hakan

doi:10.1016/j.cbi.2020.109163

Cited by 45 publications

(21 citation statements)

References 19 publications

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“…The cells were resuspended in RPMI-medium combined with Muse TM Annexin V & Dead Cell reagent and E a r l y A c c e s s maintained for 20 min at RT. Finally, apoptosis analysis was assessed with the Muse TM Cell Analyzer (Merck Millipore, Billerica, MA, USA) (17).…”

Section: Apoptosis Assaymentioning

confidence: 99%

Dosetaksel Dirençli Prostat Kanseri Hücrelerinde Timokinon Tarafından Otofajik Hücre Ölümünün İndüklenmesi

İlhan

Oğuz

2021

Düzce Tıp Fakültesi Dergisi

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Aim: Acquired docetaxel (DOC) resistance of prostate cancer (PCa) is still a clinical problem. In addition to failure in chemotherapy treatment, it causes tumor recurrence. Therefore, novel and more effective compounds are needed in DOC-resistant PCa treatment. This study aimed to investigate the possible cytotoxic and cell death-inducing activities of thymoquinone (TQ), one of the main active components of Nigella sativa L., on DOC-resistant prostate cancer cells. Material and Methods: DOC-resistant PC3 cells (DOC-R/PC3) were developed by the continuous culture with increment concentrations of DOC (1-10 nM) until they improved their growth and division abilities. The cell viability was determined by MTT assay. The Muse TM Annexin V & Dead Cell kit was performed to detect apoptotic cell death. Autophagic vacuoles were observed by staining autophagic vacuoles. The levels of LC3I, LC3II and Beclin-1 proteins were investigated via western blot analysis. Results: TQ inhibited the viability of DOC-R/PC3 cells in a dose-and time-dependent manner (p=0.014). The IC50 value of TQ for DOC-R/PC3 cells was calculated as 60 µM at 72 h. Treatment of TQ did not induce apoptotic cell death in DOC-resistant prostate cancer cells but induced the formation of autophagic vacuoles. Moreover, Beclin-1 and LC3-II protein levels were increased in TQ-treated DOC-R/PC3 cells, however, LC3-I levels were decreased in DOC-R/PC3 cells. Conclusion: All these results show that TQ may become a new therapeutic target for DOCresistant prostate cancer in the future.

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Section: Apoptosis Assaymentioning

confidence: 99%

Dosetaksel Dirençli Prostat Kanseri Hücrelerinde Timokinon Tarafından Otofajik Hücre Ölümünün İndüklenmesi

İlhan

Oğuz

2021

Düzce Tıp Fakültesi Dergisi

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“…The cytotoxic effect of Theranekron ® was evaluated via 3 -( 4 , 5 -dimethylthiazol -2 -yl ) -2 , 5diphenyltetrazolium bromide (MTT) assay [21]. Cells were seeded at 1×10 4 cells/well, in a final volume of 200 µL, in 96-well flat-bottomed plates.…”

Section: Mtt Cell Viability Assaymentioning

confidence: 99%

In vitro cytotoxic activity of Tarantula cubensis alcoholic extract on different human cell lines

Pulat

2021

Cumhuriyet Science Journal

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Spider venoms are known to have great potential for their antimicrobial, antifungal, and antitumor activities due to their rich peptide content. Tarantula cubensis alcoholic extract Theranekron ® is a homeopathic remedy and it is frequently used in veterinary treatments. Specifically, the anti-inflammatory, antitumor and wound healing effects of Theranekron ® provide a wide range of use in animal treatments. More importantly, it can reduce the growth rate of canine mammary tumors. This effect shows that Theranekron ® can be a potential candidate for cancer treatment. In this study, the cytotoxic effect of Theranekron ® was evaluated in four different human cancer cell lines and one non-cancerous human cell line. It was aimed to provide a foundation for further studies by conducting an in vitro screening for the cytotoxic effect of Theranekron ® . Results showed that Theranekron ® has a high cytotoxic effect on human breast cancer cell lines. On the other hand, the rate of cytotoxicity was found to be relatively lower on human small cell lung cancer, glioblastoma and human prostate cancer cell lines as compared to breast cancer cells. These results indicated that T. cubensis alcoholic extract might be utilized as an anticancer bio-therapeutic and should be further examined for its potential.

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“…We expect that this combination will improve the antitumor activity of such compounds and solve safety issues. For example, recent studies demonstrate that a novel series of benzimidazole derivatives have cell-cycle inhibition and apoptotic effects against a panel of selected human cancer cell lines ( Atmaca et al, 2020 ; Atmaca et al, 2021 ). The structural modification of this series of compounds holds great potential that leads to the discovery of a series of novel antitumor chemical compounds which combine the advantages of the original molecule with the introduced additional functional groups.…”

Section: Introductionmentioning

confidence: 99%

Discovery of a Series of Theophylline Derivatives Containing 1,2,3-Triazole for Treatment of Non-Small Cell Lung Cancer

Mao

Xie

et al. 2021

Front. Pharmacol.

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Chemotherapy is the most common clinical treatment for non-small cell lung cancer (NSCLC), but low efficiency and high toxicity of current chemotherapy drugs limit their clinical application. Therefore, it is urgent to develop hypotoxic and efficient chemotherapy drugs. Theophylline, a natural compound, is safe and easy to get, and it can be used as a modified scaffold structure and hold huge potential for developing safe and efficient antitumor drugs. Herein, we linked theophylline with different azide compounds to synthesize a new type of 1,2,3-triazole ring-containing theophylline derivatives. We found that some theophylline1,2,3-triazole compounds showed a good tumor-suppressive efficacy. Especially, derivative d17 showed strong antiproliferative activity against a variety of cancer cells in vitro, including H460, A549, A2780, LOVO, MB-231, MCF-7, OVCAR3, SW480, and PC-9. It is worth noting that the two NSCLC cell lines H460 H and A549 are sensitive to compound d17 particularly, with IC50 of 5.929 ± 0.97 μM and 6.76 ± 0.25 μM, respectively. Compound d17 can significantly induce cell apoptosis by increasing the ratio of apoptotic protein Bax/Bcl-2 by downregulating the expression of phosphorylated Akt protein, and it has little toxicity to normal hepatocyte cells LO2 at therapeutic concentrations. These data indicate that these theophylline acetic acid-1,2,3-triazole derivatives may be potential drug candidates for anti-NSCLC and are worthy of further study.

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Novel benzimidazole derivatives: Synthesis, in vitro cytotoxicity, apoptosis and cell cycle studies

Cited by 45 publications

References 19 publications

Dosetaksel Dirençli Prostat Kanseri Hücrelerinde Timokinon Tarafından Otofajik Hücre Ölümünün İndüklenmesi

Dosetaksel Dirençli Prostat Kanseri Hücrelerinde Timokinon Tarafından Otofajik Hücre Ölümünün İndüklenmesi

In vitro cytotoxic activity of Tarantula cubensis alcoholic extract on different human cell lines

Discovery of a Series of Theophylline Derivatives Containing 1,2,3-Triazole for Treatment of Non-Small Cell Lung Cancer

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