| Popis: |
Pancreatic cancer is the most severe among other cancers due to its late detection and less chance of survivability. Heterocycles are proven ring systems in the treatment of various cancers and this is due to the presence of two biodynamic molecules combined, have a greater synergistic efficacy in many anticancer drugs. Quinoline and pyridine ring systems are brought together to obtain greater potency and this is achieved by coupling the both using Pd-catalyst, and in the present investigation, Suzuki-Miyaura coupling (SMC) reactions are adopted to generate potent molecular entities. Pancreatic cancer is difficult to treat due to overexpression of VEGFR2 protein. VEGFR2 is targeted to design the molecules of quinoline coupled pyridine moieties and are docked to evaluate the protein ligand interaction at the binding site. The binding affinity of conjugates revealed the potency and capability of ligands to inhibit the VEGFR2 pathway. The in-silico ADMET properties were determined their inherent pharmacokinetic feasibility. The synthesised conjugates have been evaluated by MTT assay against human pancreatic cancer cell line (PANC-1). Among the series, compound 5d , 5e and 5h exhibited a greater inhibitory activity against the cell line with an IC 50 value of 82.32 , 54.74 and 80.35 µM . In the present exploration, 5e exhibited greater inhibitory activity and it could be a promising lead for the development of new chemotherapeutics against pancreatic cancer. |
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