25–26 Aug 2021 مؤتمر
كلية الصيدلة
Asia/Baghdad timezone

New picolinic acid derivatives: Synthesis, docking study and anti-EGFR kinase inhibitory effect

Not scheduled
15m
كلية الصيدلة

كلية الصيدلة

(Virtual)
Live presentation Track Three (August 26th, 5-7 PM)

Speaker

Dr Ali H. Abbas (Department of Pharmaceutical Chemistry, College of Pharmacy, University of Tikrit, Salah-Aldin 34001, Iraq)

Description

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 mg/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 mM) which was supported by the molecular docking studies that showed compound 4C might be considered as a potential inhibitor of EGFR kinase.

Has the manuscript been published? published
Journal name , year , Volume, Issue and Article link Materials Today: Proceedings. 2021 May 31. https://www.sciencedirect.com/science/article/pii/S2214785321039535. https://doi.org/10.1016/j.matpr.2021.05.354
Journal name Materials Today: Proceedings

Primary author

Dr Ali H. Abbas (Department of Pharmaceutical Chemistry, College of Pharmacy, University of Tikrit, Salah-Aldin 34001, Iraq)

Co-authors

Ammar A. Razzak Mahmood (Department of Pharmaceutical Chemistry, College of Pharmacy, University of Baghdad, Baghdad, Bab-Al-Mouadam-10001, Iraq) Prof. Lubna H. Tahtamouni (Department of Biochemistry and Molecular Biology, College of Natural Sciences, Colorado State University, Fort Collins, CO, USA) Zainab A. Al-Mazaydeh (Department of Biology and Biotechnology, Faculty of Science, the Hashemite University, Zarqa, Jordan) Ms Majdoleen S. Rammaha (Department of Biology and Biotechnology, Faculty of Science, the Hashemite University, Zarqa, Jordan) Ms Fatima Alsoubani (Department of Chemistry, Faculty of Science, the Hashemite University, Zarqa, Jordan) Prof. Rheda I. Al-bayati (Department of Chemistry, College of Science, Al-Mustansirya University, Baghdad 10001, Iraq)

Presentation materials

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