Ligand substituent effect on the cytotoxicity activity of two new copper(<scp>ii</scp>) complexes bearing 8-hydroxyquinoline derivatives: validated by MTT assay and apoptosis in MCF-7 cancer cell line (human breast cancer)

Ali, Amjad; Banerjee, Somesh; Kamaal, Saima; Usman, Mohammad; Das, Neeladrisingha; Afzal, Mohd; Alarifi, Abdullah; Sepay, Nayim; Roy, Partha; Ahmad, Musheer

doi:10.1039/d1ra00172h

Cited by 35 publications

(14 citation statements)

References 54 publications

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“…Isatin, when attached with thiazoles (Figure 2E), exhibited remarkable anti-HIV activity and were disclosed as HIV reverse transcriptase dual inhibitors [22]. Hydrazonoindolin-2one derivatives are considered safer anticancer drugs for their anti-proliferative activity against human adenocarcinoma (A-549), human colorectal adenocarcinoma (HT-29), and human breast carcinoma (ZR-75) cell lines [23,24]. Besides antiviral [25,26] and tuberculostatic [27] activities, various isatin derivatives have been reported for anticancer and cytotoxic activities [28][29][30][31][32].…”

Section: Introductionmentioning

confidence: 99%

Investigations on Anticancer Potentials by DNA Binding and Cytotoxicity Studies for Newly Synthesized and Characterized Imidazolidine and Thiazolidine-Based Isatin Derivatives

et al. 2022

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Imidazolidine and thiazolidine-based isatin derivatives (IST-01–04) were synthesized, characterized, and tested for their interactions with ds-DNA. Theoretical and experimental findings showed good compatibility and indicated compound–DNA binding by mixed mode of interactions. The evaluated binding parameters, i.e., binding constant (Kb), free energy change (ΔG), and binding site sizes (n), inferred comparatively greater and more spontaneous binding interactions of IST-02 and then IST-04 with the DNA, among all compounds tested under physiological pH and temperature (7.4, 37 °C). The cytotoxic activity of all compounds was assessed against HeLa (cervical carcinoma), MCF-7 (breast carcinoma), and HuH-7 (liver carcinoma), as well as normal HEK-293 (human embryonic kidney) cell lines. Among all compounds, IST-02 and 04 were found to be cytotoxic against HuH-7 cell lines with percentage cell toxicity of 75% and 66%, respectively, at 500 ng/µL dosage. Moreover, HEK-293 cells exhibit tolerance to the increasing drug concentration, suggesting these two compounds are less cytotoxic against normal cell lines compared to cancer cell lines. Hence, both DNA binding and cytotoxicity studies proved imidazolidine (IST-02) and thiazolidine (IST-04)-based isatin derivatives as potent anticancer drug candidates among which imidazolidine (IST-02) is comparatively the more promising.

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Section: Introductionmentioning

confidence: 99%

Investigations on Anticancer Potentials by DNA Binding and Cytotoxicity Studies for Newly Synthesized and Characterized Imidazolidine and Thiazolidine-Based Isatin Derivatives

et al. 2022

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“…The cytotoxicity of compounds 1a , 2c , and 2f toward the HL-7702 human cell line was evaluated by an MTT assay. , Briefly, cells were cultivated at a density of 1 × 10 5 cells/mL in 96-well plates at 37 °C with 5% (v/v) CO 2 for 1 day. Then, 10 μL of DMSO and PBS solution of test compounds was injected to explore the cell viability.…”

Section: Methodsmentioning

confidence: 99%

Synthesis, Structure–Activity Relationship, and Mechanism of a Series of Diarylhydrazide Compounds as Potential Antifungal Agents

Liu

et al. 2023

J. Agric. Food Chem.

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A series of simple diarylhydrazide derivatives (45 examples) were well-designed, prepared, and screened for their antifungal activities both in vitro and in vivo. Bioassay results suggested that all designed compounds had significant activity against Alternaria brassicae (EC 50 = 0.30−8.35 μg/mL). Among of them, 2c, as the highest activity compound, could effectively inhibit the growth of plant pathogens Pyricularia oryza, Fusarium solani, Alternaria solani, Alternaria brassicae, and Alternaria alternate and was more potent than carbendazim and thiabendazole. 2c showed almost 100% protection at 200 μg/mL in vivo activity against A. solani in tomato. Moreover, 2c did not affect the germination of cowpea seed and the growth of normal human hepatocytes. The preliminary mechanistic exploration documented that 2c could result in the abnormal morphology and irregular structure of the cell membrane, destroy the function of mitochondria, increase the reactive oxygen species, and inhibit the proliferation of hypha cell. The above results manifested that target compound 2c could be a potential fungicidal candidate against phytopathogenic diseases for its excellent fungicidal activities.

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“…The in-vitro cytotoxicity of the complexes [CuL1], [CuL2] and [CuL3] was assessed by the 3-[4,5-dimethylthiazol-2-yl] 2,5diphenyltetrazolium bromide (MTT) assay [84,85] against MCF7 breast cancer cell lines. The yellow tetrazolium salt MTT is water soluble succinate-dehydrogenase, a mitochondrial enzyme found in live cells, that breaks the tetrazolium ring, turning the MTT into an insoluble purple formazan.…”

Section: Mtt Assaymentioning

confidence: 99%

1‐Benzyl‐1H‐indazol‐3‐ol Copper(II) Derivatives as Anticancer Agents: In‐vitro Interaction with DNA/BSA, DFT, Molecular Docking and Cytotoxicity on MCF7 Cells

Salimath,

Pathak

2024

ChemistrySelect

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A set of three copper(II) complexes C28H24CuN4O2 [CuL1], C24H22CuN4O [CuL2] and C26H22CuN4O [CuL3] incorporated with ligands 1‐benzyl‐1H‐indazol‐3‐ol, 2,2′‐bipyridyl and 1,10‐phenanthroline have been synthesized, characterized and subjected for biomedical applications. New copper(II) derivatives were characterized by FTIR, EPR and HRMS spectral tools. Cyclic voltammograms were recorded to ascertain redox potential and UV‐Vis and Fluorometer were employed to establish photophysical properties of all the new copper(II) complexes. Further, these derivatives of Cu(II) were subjected for DNA and BSA binding studies by using absorption‐emission spectral methods and viscosity measurements as well as by molecular docking. DFT studies of the above‐mentioned derivatives suggested square planar geometry along with other relevant molecular investigations. Eventually, these new Cu(II) complexes have been tested with DPPH and MTT assay to determine the cytotoxicity against MCF7 cell lines to observe remarkable potency with IC50 values 80.68 μg/ml, 49.40 μg/ml and 45.91 μg/ml, respectively.

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Ligand substituent effect on the cytotoxicity activity of two new copper(ii) complexes bearing 8-hydroxyquinoline derivatives: validated by MTT assay and apoptosis in MCF-7 cancer cell line (human breast cancer)

Abstract: The presence of –COOH functionality in a copper(ii) complex leads to higher cytotoxicity than that observed for a complex containing a –CN group.

Cited by 35 publications

References 54 publications

Investigations on Anticancer Potentials by DNA Binding and Cytotoxicity Studies for Newly Synthesized and Characterized Imidazolidine and Thiazolidine-Based Isatin Derivatives

Investigations on Anticancer Potentials by DNA Binding and Cytotoxicity Studies for Newly Synthesized and Characterized Imidazolidine and Thiazolidine-Based Isatin Derivatives

Synthesis, Structure–Activity Relationship, and Mechanism of a Series of Diarylhydrazide Compounds as Potential Antifungal Agents

1‐Benzyl‐1H‐indazol‐3‐ol Copper(II) Derivatives as Anticancer Agents: In‐vitro Interaction with DNA/BSA, DFT, Molecular Docking and Cytotoxicity on MCF7 Cells

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