الفهرس 
introduction (literature reviewOnly 14 pages are availabe for public view
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Abstract
The present study was proposed to combine tetrazole and chalcone pharmacophores in new derivatives, and then extended to get new tetrazole-pyrazoline integrated compounds. Hence, we describe the synthesis of new hybrid molecules, by incorporating the tetrazole nucleus and chalcone / pyrazoline moieties in a single structure, to be evaluated as anti-proliferative compounds. The results and discussion of the synthesis of the designed compounds by different routes were presented via four schemes. Also, discusses the in vitro anti-proliferative activities of the prepared compounds on different mammalian cell lines: colon cancer cell line (HCT-116), prostate cancer cell line (PC-3), breast cancer cell line (MCF-7) and normal cell line of the African green monkey kidney cells (Vero-B) using MTT assay validation. The molecular docking simulation was performed to explore the binding interactions of some of the prepared compounds with different enzymes involved in cell proliferation. The selected enzymes are histone deacetylase 2 (HDAC2), cytochrome P450 17A1 (CYP17A1) and 5,10-methenyltetrahydrofolate synthetase (MTHFS). Finally, a concise conclusion of the work showed that the biological results indicated the anti-proliferative activity reside in the tetrazole-chalcone hybrids, rather than in their corresponding pyrazoline derivatives. Ten of the tested chalcone compounds showed promising anti-proliferative activities with better or equal IC50 values than that of the reference drugs, cisplatin and 5-FU, against the tested HCT-116, with variable activities against the other tested cell lines PC-3 and MCF-7 and with high selectivity. Only one pyrazoline compound showed a broad spectrum of activity, by exhibiting potency against the three tested cell lines.