الفهرس | Only 14 pages are availabe for public view |
Abstract Chapter I (Introduction): An introductory part describing the chemistry of thienopyrimidine, different approaches for its synthesis and c-Kit/PDGFR-α dual inhibitors as targeted chemotherapeutic agents such as imatinib, telatinib, tivozanib and amuvatinib. Chapter II (Research Objectives): The aim of this research is to synthesize novel c-Kit/PDGFR-α dual inhibitors as structural analogues of amuvatinib and evaluate their cytotoxic effect on pancreatic cancer cell line (PANC-1). Our strategy is directed toward the design of a variety of ligands by replacing benzofuro[3,2-d]pyrimidine of amuvatinib with thieno[2,3-d]pyrimidine derivatives in the hope of discovering more active ATP site inhibitors. Chapter III (Theoretical Discussion): Synthetic pathways that have been followed to obtain final new compounds and their mechanisms, spectral data, biological results and molecular modeling. Chapter IV (Experimental): A number of new thieno[2,3-d]pyrimidine derivatives were synthesized. The potential cytotoxicity of the synthesized compounds was tested on PANC-1 using Skehan methodology. Docking study for the most active derivatives was carried out on the crystal structure of both PDGFR-α and c-Kit. Chapter V (Conclusion): A summary of the present study and conclusions. Chapter VI (References): A list of references which were used and their arrangement according to their order in the thesis. |