Cytotoxic and apoptosis inducing effect of some pyrano [3, 2-c] pyridine derivatives against MCF-7 Breast Cancer Cells

Rahnamay, Mohammad; Mahdavi, Majid; Shekarchi, Ali Akbar; Zare, Payman; Feizi, Mohammad Ali Hosseinpour

doi:10.18388/abp.2017_1629

Cited by 16 publications

(4 citation statements)

References 24 publications

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“…Further cell cycle analysis, A.O./Et.Br. double staining and DNA fragmentation assay proved that compound 33 exerted its anti-proliferative activity by apoptosis induction in MCF-7 cells [57]. 5) as potential aromatase inhibitors.…”

Section: Pyridine and Fused Pyridine Derivativesmentioning

confidence: 94%

Recent Advancements in the Development of Anti-Breast Cancer Synthetic Small Molecules

Elkaeed

Salam²,

Sabt³

et al. 2021

Molecules

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Among all cancer types, breast cancer (BC) still stands as one of the most serious diseases responsible for a large number of cancer-associated deaths among women worldwide, and diagnosed cases are increasing year by year worldwide. For a very long time, hormonal therapy, surgery, chemotherapy, and radiotherapy were used for breast cancer treatment. However, these treatment approaches are becoming progressively futile because of multidrug resistance and serious side effects. Consequently, there is a pressing demand to develop more efficient and safer agents that can fight breast cancer belligerence and inhibit cancer cell proliferation, invasion and metastasis. Currently, there is an avalanche of newly designed and synthesized molecular entities targeting multiple types of breast cancer. This review highlights several important synthesized compounds with promising anti-BC activity that are categorized according to their chemical structures.

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Section: Pyridine and Fused Pyridine Derivativesmentioning

confidence: 94%

Recent Advancements in the Development of Anti-Breast Cancer Synthetic Small Molecules

Elkaeed

Salam²,

Sabt³

et al. 2021

Molecules

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“…The cytotoxicity of Cu(L) 2 and Cu(AZ) 2 was further established by colony formation assay using MCF7 cells by using our previously standardized protocol. 57 Cells were seeded at 500 cells in 2 ml/well (low density) for the assay in a six-well plate and were treated with Cu(L) 2 and Cu(AZ) 2 and incubated for 24 h. After fixing and staining with Gram's crystal violet solution, the numbers of colony were counted in treated cell line. All the statistical analysis was carried out with the help of GraphPad Prism 8.0.…”

Section: Colony Formation Assaymentioning

confidence: 99%

High anticancer activity in short response time exhibited by a new azobenzene derivative and its copper complex

Dev,

Mitra,

Sinha

et al. 2024

Applied Organom Chemis

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o‐Aminoazotoluene (OAT), capable of photoisomerization, and o‐vanillin, a potent comutagen, have been used to synthesize a new ligand, HL, [C6H4(CH3)N=NC6H3(CH3)N=CHC6H3(OH)(OCH3)], which, upon complexation with copper(II), results in a new copper(II) complex‐Cu(L)2, [Cu{C6H4(CH3)N=NC6H3(CH3)N=CHC6H3(OCH3)O}2]. Both HL and Cu(L)2 have been characterized by single‐crystal X‐ray diffraction measurements along with other analytical techniques, for example, IR spectroscopy, NMR spectroscopy, UV–Vis spectroscopy, elemental analysis and mass spectrometry. These compounds were tested with different in vitro anticancer assay as well as with in silico studies. A comparative study has been demonstrated on anticancer activity of HL and Cu(L)2 with the ligand HAZ, {C6H5N=NC6H4N=CHC6H3(OH)(OCH3)} and its Cu‐complex, [Cu(AZ)2, Cu{C6H5N=NC6H4N=CHC6H3(OCH3)O}2]. The sensing properties of HAZ, along with the synthesis and structural properties of both HAZ and Cu(AZ)2, have been reported by our group earlier. Cytotoxicity measurements on MCF7 cell lines show that Cu(L)2 and Cu(AZ)2 have higher anticancer activity than their corresponding ligands. The apoptotic effect of Cu‐complex was studied through nuclear fragmentation assay and AO/EB dual‐staining assay on MCF7 cell line. The IC50 value of Cu(L)2 in 0.01% DMSO/water after 24‐h treatment was found 4.2 μM, which is one of the lowest values with this response time compared to the other analogous anticancer compounds. Finally, we have evaluated the expression of hERα protein with respect to Cu‐complexes, and it was observed that Cu(L)2 caused more down‐regulation of hERα as compared to Cu(AZ)2.

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“…These functional groups exhibit cytotoxic and anti-proliferative properties against various cancer cells through the activation of the apoptosis pathway, as demonstrated in studies involving 2-methylpyridine-1-ium-1-sulfonate, pyrano[3,2-c]pyridines, and their derivatives. These compounds have been identified as potent suppressors of HBC cell lines and robust inducers of apoptosis [38,39]. Moreover, some BZOP derivatives were reported to exhibit anticancer activity against a human colorectal cancer cell line (HCT-116) with a low IC 50 value [40].…”

Section: Introductionmentioning

confidence: 99%

A New Benzo[6,7]oxepino[3,2-b] Pyridine Derivative Induces Apoptosis in Canine Mammary Cancer Cell Lines

Jianpraphat,

Supsavhad,

Ngernmeesri

et al. 2024

Animals

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CMC is the most frequently diagnosed cancer and one of the leading causes of death in non-spayed female dogs. Exploring novel therapeutic agents is necessary to increase the survival rate of dogs with CMC. MPOBA is a BZOP derivative that has a significant anticancer effect in a human cell line. The main goal of this study was to investigate the anticancer properties of MPOBA against two CMC cell lines (REM134 and CMGT071020) using a 3-(4,5-Dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay, a wound healing assay, a transwell migration assay, an Annexin V-FITC apoptosis assay with a flow cytometry analysis, a mRNA expression analysis using quantitative real-time PCR (qRT-PCR), and an immunohistochemistry (IHC). According to the accumulated studies, MPOBA caused significant concentration- and time-dependent reductions in cell proliferation and cell migration and induced apoptosis in both CMC cell lines. In gene expression analysis, nine canine genes, including TP53, BCL-2, BAX, epidermal growth factor receptor (EGFR), snail transcription factor (SNAIL), snail-related zinc-finger transcription factor (SLUG), TWIST, E-cadherin, and N-cadherin, were investigated. The mRNA expression results revealed that MPOBA induced upregulation of TP53 and overexpression of the pro-apoptotic gene BAX, together with an inhibition of BCL-2. Moreover, MPOBA also suppressed the mRNA expression levels of SNAIL, EGFR, and N-cadherin and induced upregulation of E-cadherin, crucial genes related to the epithelial-to-mesenchymal transition (EMT). However, there was no significant difference in the IHC results of the expression patterns of vimentin (VT) and cytokeratin (CK) between MPOBA-treated and control CMC cells. In conclusion, the results of the present study suggested that MPOBA exhibited significant anticancer activity by inducing apoptosis in both CMCs via upregulation of TP53 and BAX and downregulation of BCL-2 relative mRNA expression. MPOBA may prove to be a potential candidate drug to be further investigated as a therapeutic agent for CMC.

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Cytotoxic and apoptosis inducing effect of some pyrano [3, 2-c] pyridine derivatives against MCF-7 Breast Cancer Cells

Cited by 16 publications

References 24 publications

Recent Advancements in the Development of Anti-Breast Cancer Synthetic Small Molecules

Recent Advancements in the Development of Anti-Breast Cancer Synthetic Small Molecules

High anticancer activity in short response time exhibited by a new azobenzene derivative and its copper complex

A New Benzo[6,7]oxepino[3,2-b] Pyridine Derivative Induces Apoptosis in Canine Mammary Cancer Cell Lines

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