Synthesis and screening of anti-cancer,antioxidant, and anti-inflammatory activities of novel galloyl pyrazoline derivatives |
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Authors: | Mohamed Abdel-Aziz |
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Affiliation: | Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, Egypt |
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Abstract: | A novel series of galloyl-2-pyrazoline derivatives were synthesized and screened for their cytotoxic effect against hepatocellular carcinoma (Hep-G2) and colon carcinoma (HCT-116) cells using the MTT assay, proliferative effect on the immune cells RAW macrophage 264.7 using the MTT assay, anti-inflammatory activity through measurement of the accumulation of nitrites using Griess reagent, and for their antioxidant activity through scavenging of the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical. Most of the tested compounds had a concomitant weak cytotoxic effect against both Hep-G2 and HCT-116 cells, except 5-(2-furyl)-4,5-dihydro-1-(3,4,5-trihydroxybenzoyl)-3-(3,4-dimethoxyphenyl)-1H-pyrazole (IC50 8.4 μg/mL and 18.6 μg/mL) and 5-(4-cyanophenyl)-4,5-dihydro-1-(3,4,5-trihydroxybenzoyl)-3-(3,4-dimethoxy-phenyl)-1H-pyrazole (IC50 15.2 μg/mL, 31.5 μg/mL), which exhibited a cytotoxic effect against Hep-G2 and HCT-116 cells, respectively, while only 5-(2,6-dichlorophenyl)-4,5-dihydro-1-(3,4,5-trihydroxybenzoyl)-3-(3,4-dimethoxyphenyl)-1H-pyrazole was a significant dose-dependent inducer of macrophage proliferation. On the other hand, all of the tested compounds were significant inhibitors of LPS-stimulated NO generation and potential scavengers of the DPPH radical, except 1-(3,4,5-trihydroxybenzoyl)-4,5-dihydro-5-(4-methoxyphenyl)-3-(3,4-dimethoxyphenyl)-1H-pyrazole. |
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Keywords: | 2-Pyrazoline galloyl derivatives anti-cancer anti-inflammatory antioxidant |
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