Abstract
Abstract New derivatives (4A-4D) were designed and synthesized from, picolinic acid (PA). The newly synthesized compounds were confirmed by ATR-FTIR, 1HNMRS, 13CNMR and CHNS analysis. The molecular docking methodology of (4A-4D) against EGFR kinase revealed that certain compounds occupied the vital site of EGFR kinase pocket and with a good fit. By employing the MTT assay, it was found that. compound 4C has anti-tumor activity against MCF-7 breast cancer cell line (GI50 = 86.8 µg/mL), but not against the A549 lung cancer cell line or normal cells (MCF10A and WBC). Compound 4C caused MCF-7 cell death by apoptosis as visualized by fragmented nuclei and smeared genomic DNA. Furthermore, compound 4C increased caspase 9 mRNA levels and caused its activation. Additionally, compound 4C-treated MCF-7 cells showed enhanced cytochrome -c- release from a mitochondria to the cytosol, reflecting the initiation of the intrinsic apoptotic pathway. Finally, compound 4C exhibited EGFR kinase inhibitory activity (7.15 µM) which was supported by the molecular docking studies that showed compound 4C might be considered as a potential inhibitor of EGFR kinase.
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