Design, synthesis and antitumor activity of new aza heterocyclic derivatives / Riham Ismail Ahmed ; Supervised Samir M. Elmoghazy , Fadi M. Awadallah

Thesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry

Herein, we reported the synthesis and cytotoxic activity of two classes of compounds. The first one included the appropriately substituted 4,6-diphenyl cyclohexenone derivatives III , VI , VII , VIII and IX bearing at position 1 a,b a,b a,b a,b a-f functional moieties contributing to cytotoxic activity such as hydrazide, oxadiazole, pyrazole and thiosemicarbazide, respectively. The second class of compounds IV a,b and V featured a 3-hydroxy-indazole core as a cyclic rigid substitute for the a-f 1-thiosemicarbazide moiety on the cyclohexenone nucleus of the first group IX .a-f Twenty-four new compounds were tested for their antiproliferative activity using the MTT assay against human colon cell line (HCT-116) and breast cancer cell line (MCF-7) at Vacsera, Egypt. The active compounds were investigated for their mechanism of action as tubulin polymerization inhibitors. Molecular modeling was performed to assess the binding of the active compounds

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