Synthesis and biological evaluation of some new nitrogen heterocyclic compounds / Islam Zaki Abdelazeem Abutaleb ; Supervised Mohammed Kamal Abdelhameid , Khaled Omar Ahmed Mohamed , Ibrahim Elsayed Mohey Eldeen

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

A new series of diamide, imidazolone, 1,2,4-triazole and 1,2,4-triazinone derivatives have been designed, synthesized starting from N-benzoylglycine derivatives. Structures of the synthesized compounds have been deduced on the basis of their spectroscopic methods and elemental analyses data. The in vitroantitumor activity of the newly synthesized compounds were screenedagainstHepG2 and MCF-7 cell lines. Cell cycle analysis were carried out for some of the prepared compounds and demonstrated cell cycle arrest at G1 or G2/M phases of cell cycle.Additionally, the compounds produced a significant reduction in cellular microtubules for microtubule loss and potently inhibited the binding of [3H]colchicine to tubulin. Finally, some of the prepared compounds were proved to upregulate expression of proteins triggering apoptosis such as p53, Bax and decreased Bcl-2 overexpression as well as increased the expression of effector caspase-3/7.

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