الإشراف على رسائل الماجستير
Synthesis characterization and biological evaluation of benzamide derivatives
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Sarah Alhababseh Alazaydeh
Cancer is a life-threatening disease that results from a defect in the cell cycle that leads to uncontrollably divided cancer cells caused by genetic changes. Cancer is expected to become the most common cause of death within the next few years. The benzamide derivatives have attracted scientists because of their broad biological activity. Modification applied on benzamide structure produces several benzamide derivatives with variable biological activities such as antioxidant, anticancer, antibacterial, antifungal, anti-inflammatory. The goal of this study was to synthesis benzamide derivatives and assess their in vitro cytotoxicity against two cell lines: the human colorectal cancer (HT-29) cell line and breast adenocarcinoma (MCF-7) cell line. The 2- aminobenzamide and acyl chlorides were directly coupled to create these compounds in anhydrous tetrahydrofuran (THF) without the need of a catalyst. The bulk of the compounds were synthesized with good yield range (80.7-85.2%), and nuclear magnetic resonance (NMR), Fourier transform infrared spectroscopy (FTIR), gas chromatography-mass spectroscopy (GC-MS), and liquid chromatography-mass spectroscopy (LC-MS) all confirmed the structures of the compounds. After that, the compounds were examined in vitro utilizing the MTT assay test, which required three trials for each substance compounds 2, 3 and 4 along with doxorubicin (as a reference drug). In the studied concentration range (0.005-500 µM), Compound 3 displays strongest cytotoxic activity than 2 and 4 against the breast adenocarcinoma (MCF-7) cell lines, with an IC50 value 0.8331, 7.85 and 84.73 µM, respectively. Compounds 2, 3 and 4 don't have any cytotoxic effects on human colorectal cancer (HT-29) cell lines in the concentration range (0.0005-500 µM) where they were evaluated. Our results suggested that compounds 2, 3 and 4 may act as a fundamental scaffold for developing future anticancer medicines with effective structural design.