الفهرس 
Design, synthesis and antitumor activity of some novel pyrazoline derivatives
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Abstract
Cancer is the second cause of death after cardiac diseases worldwide. It is continuing to act as the main health problem in both developing and developed countries. Therefore, there is an incessant need to search for new anticancer agents that inhibit new targets leading to more effectiveness and less side effects compared to the conventional chemotherapy.Literature review showed that pyrazoline derivatives display a therapeutic activity as anticancer agents against breast, colon, lung, liver, cervical cancer by different mechanisms of action through acting on variable targets.Accordingly, the present study is concerned with the synthesis of some derivatives belonging to the 1,3,5-trisubstituted pyrazolines IIa-c, IIIa-c, IVa-f, VIa-c, VIIa-f, VIIIa-f, IXa,b. This is achieved via the intermediates (1E,4E)-1,5-Diphenylpenta-1,4-dien-3-one (Ia), (1E,4E)-1,5-Bis(4-chloro-phenyl) penta-1,4-dien-3-one (Ib), (1E,4E)-1,5-Bis(4-methoxyphenyl)penta-1,4-dien-3-one (Ic), (2E,4E)-1,5-Diphenylpenta-2,4-dien-1-one (Va), (2E,4E) -1-(4-Chlorophenyl)-5-phenylpenta-2,4-dien-1-one (Vb) and (2E,4E)-1-(4-Methoxyphenyl)-5-phenylpenta-2,4-dien-1-one (Vc).The newly synthesized compounds were evaluated for their in vitro cytotoxicity against human breast cancer cell line (MCF-7) in addition to normal fibroblast cell (WI38) using staurosporine and erlotinib as reference standards. Compounds eliciting superior anticancer activity were screened for their EGFR inhibitory activity and were compared to erlotinib. Moreover, Molecular docking simulations were performed on compounds revealing significant EGFR inhibitory activity to investigate their binding mode in the active site of the enzyme