Synthesis and anticancer properties of some novel Cyanopyridines-based hybrid molecules bearing pyrazole, oxadiazole, and N-acylhydrazone moieties.

Abstract

In order to decrease the level of toxicity and improve the selectivity of drugs toward cancer targets, hybrid drugs are designed to simultaneously modulate multiple targets of multifactorial diseases to overcome the side effects associated with a single target-drugs. As a result, the development of hybrid molecules has become the centre of research. Owing to the pharmacological data of pyridine, 1,3,4 oxadiazole, and pyrazole rings, we are interested in synthesizing new hybrid molecules and examining their anti-cancer activities. In the first chapter of the manuscript, a bibliographical study described the biological interests and synthesis methods of four heterocyclic systems, namely cyanopridines, pyrazoles, oxadiazoles, and N-acylhydrazones. In the second chapter, we developed novel conditions to prepare a well-furnished library of acetohydrazides from cyanopyridones as starting materials. The reactivity of the formers was used to synthesize three novel series bearing pyarzoles, 1,3,4 oxadiazoles, and hydrazones containing isatin moieties. in the final chapter of the thesis, as the main objective, was evaluating and discussing the synthesized molecules' anticancer properties against different cancer cell lines (A‐2780, MCF‐7, and Caco-2) using MTT assay.