Abstract
Abstract The present study aimed to design and synthesize a series of phenyl-isoxazole-carboxamide derivatives and investigate their antitumor and antioxidant activities. The in vitro cytotoxic evaluation was conducted using the MTS assay against four cancer cell lines: hepatocellular carcinoma (Hep3B and HepG2), cervical adenocarcinoma (HeLa), breast carcinoma (MCF-7), in addition to the normal cell line (Hek293T). Besides, the antioxidant activity was evaluated using a 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. All obtained compounds were found to have potent to moderate activities against Hep3B and MCF-7 cancer cells lines, except compound 2e. It was found that compound 2a has potent activity against HeLa and Hep3B cancer cell lines with IC50 values of 0.91 and 8.02 µM, respectively. The IC50 dose range of the tested compounds against Hep3B was 5.96–28.62 µM, except for 2e, compared with doxorubicin, which has an IC50 value of 2.23 µM. Also, the IC50 value range of the compounds against Hek293T was 112.78–266.66 µM, compared with doxorubicin, which has an IC50 dose of 0.581 µM. The antioxidant activity of the synthesized compounds was weak, and compound 2d showed moderate activity against the DPPH enzyme with an IC50 value of 138.50 µM in comparison with Trolox, which has an IC50 dose of 37.23 µM.
Highlights
In 2020, worldwide cancer disease was the leading cause of death, which accounted for about 10 million deaths
In 2018, about 13% of patients diagnosed with cancer were associated with carcinogenic infections, including Epstein-Barr virus, hepatitis C virus, hepatitis B virus, human papillomavirus (HPV), and Helicobacter pylori [3,4]
The current work aims to synthesize a series of isoxazole-carboxamide derivatives (2a–2e) with or without a methoxyphenyl moiety, characterization of their chemical structures with IR, 1H-NMR, and 13C-NMR spectroscopy, predict their bioactivity score by molinspiration analysis and evaluating their anti-proliferative activity against four cancer cell lines, liver (Hep3B, HepG2), cervical (HeLa), and breast (MCF-7) comparing with normal cell line (Hek293T), as well as antioxidant activity was evaluated using the DPPH assay (2,2′-diphenyl-1-picrylhydrazyl radical)
Summary
In 2020, worldwide cancer disease was the leading cause of death, which accounted for about 10 million deaths. A series of isoxazole derivatives were synthesized and evaluated as antioxidant agents One of these structures (Figure 1: St.4) has potent antioxidant activity with an IC50 value of 7.8 ± 1.21 μg/mL, compared with Trolox as a positive control (IC50: 2.75 μg/mL) [20]. The current work aims to synthesize a series of isoxazole-carboxamide derivatives (2a–2e) with or without a methoxyphenyl moiety, characterization of their chemical structures with IR, 1H-NMR, and 13C-NMR spectroscopy, predict their bioactivity score by molinspiration analysis and evaluating their anti-proliferative activity against four cancer cell lines, liver (Hep3B, HepG2), cervical (HeLa), and breast (MCF-7) comparing with normal cell line (Hek293T), as well as antioxidant activity was evaluated using the DPPH assay (2,2′-diphenyl-1-picrylhydrazyl radical)
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