Design and synthesis of certain new pyridine, pyrimidine and benzimidazole containing compounds with cytotoxic activity / Noha Ryad Mohamed Mohamed Gabr ; Supervised Mohamed Mohsen Ismail , Salwa Elsayed Mohamed Elmeligie , Mohammed Kamal Abdelhamid

Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Organic Chemistry

The present thesis composed of five chapters in which a new series of pyridine, pyrimidine and benzimidazole derivatives was designed and synthesized as potential antitumor molecules. The first chapter is an introduction which consists of a brief survey on the different methods of synthesis of pyridine, pyrimidine and benzimidazole derivatives and some of their useful biological activities. The second chapter explains the aim of the work and Schemes that have been carried out to obtain the new target pyridine, pyrimidine and benzimidazole derivatives The third chapter clarifies the theoretical discussion of the experimental work that has been carried out for the preparation of the target compounds IVa-XIXa-c as well as discussion of their spectral data. Additionally, a brief account on the docking study that explained the biological results through the binding conformations of the new compounds in comparison with the lead. The fourth chapter represents the experimental part of this work, which contains the detailed procedures used for the synthesis of the starting materials and the target pyridine and pyrimidine derivatives IVa-VIa-d as well as benzimidazole derivatives IXXIXa- c. Moreover, this chapter includes detailed spectral analysis, physical properties as well as elemental analysis of these compounds. It has been also shed the light on the cytotoxic activities of the newly synthesized pyridine and pyrimidine derivatives IVa-VIa-d in comparison with combretastatin-A-4 (CA-4) as a standard cytotoxic agent and benzimidazole derivatives IXa-XIXa-c in comparison with campetothecin (CPT)as a standard cytotoxic agent

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