2021
DOI: 10.1111/cbdd.13997
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Quinoline‐based thiazolidinone derivatives as potent cytotoxic and apoptosis‐inducing agents through EGFR inhibition

Abstract: Quinoline-based thiazolidinone heterocycles exhibited potent activity in the field of cancer therapy. Hence, ten quinoline-based thiazolidinone derivatives were evaluated for their anticancer activity through cytotoxic activity, epidermal growth factor receptor (EGFR) inhibition pathway, apoptosis investigation through flow cytometric analyses, RT-PCR gene expression, in vivo solid-Ehrlich carcinoma model, and finally in silico approach for highlighting the interaction pose. Results revealed that compound 7 ex… Show more

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Cited by 27 publications
(19 citation statements)
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“…As cyclic-dependent kinase (CDK-2) and epidermal growth factor receptor (EGFR) are key proteins that mediate and trigger the proliferation of cancer cells, their inhibition is an interesting target for apoptosis induction upon treatment of a chemotherapeutic drug. A molecular docking study was performed to highlight the virtual mechanism of binding toward EGFR and CDK-2 proteins. As seen in Figure , compound 3b was docked inside the EGFR binding site with the binding energy of −19.63 kcal/mol, and it formed one H-bind interaction with Met 769 as the H-bond acceptor.…”
Section: Resultsmentioning
confidence: 99%
“…As cyclic-dependent kinase (CDK-2) and epidermal growth factor receptor (EGFR) are key proteins that mediate and trigger the proliferation of cancer cells, their inhibition is an interesting target for apoptosis induction upon treatment of a chemotherapeutic drug. A molecular docking study was performed to highlight the virtual mechanism of binding toward EGFR and CDK-2 proteins. As seen in Figure , compound 3b was docked inside the EGFR binding site with the binding energy of −19.63 kcal/mol, and it formed one H-bind interaction with Met 769 as the H-bond acceptor.…”
Section: Resultsmentioning
confidence: 99%
“…The percentage inhibition of autophosphorylation by substances was estimated using the following equation: . 107,108…”
Section: Methodsmentioning
confidence: 99%
“…The cells were suspended in 100 µL of annexin-binding buffer solution “25 mM CaCl 2 , 1.4 M NaCl, and 0.1 M Hepes/NaOH, pH 7.4” and incubated with “Annexin V-FITC solution (1:100) and propidium iodide (PI)” at a concentration equal 10 µg/mL in the dark for 30 min. Stained cells were then obtained by a Cytoflex FACS machine, and data analysis was performed using cytExpert software [ 71 , 72 , 73 ].…”
Section: Methodsmentioning
confidence: 99%