Quinoline-based thiazolidinone derivatives as potent cytotoxic and apoptosis-inducing agents through EGFR inhibition.

Chemical Biology & Drug Design
Mohamed S NafieAtef M Amer

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 exhibited cytotoxic activity against HCT-116 cells with an IC50 value of 7.43 µM compared to 5-FU (IC50  = 11.36 µM) with moderate cytotoxic activity against the FHC (IC50  = 35.27 µM), and it exhibited remarkable inhibition activity of EGFR with IC50 value of 96.43 nM compared to Erlotinib (IC50  = 78.65 nM). Moreover, it significantly stimulated apoptotic colon cancer cell death with 171.58-fold arresting cell cycle at G2 and S-phases. Additionally, it ameliorated both biochemical and histochemical structures near normal with tumor inhibition ratio of 52.92% compared to 5-FU of 57.16%, with immunohistochemical examinations of EGFR inhibition in the treated group compared to control. Finally, molecular docking study highlig...Continue Reading

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