期刊
ACS OMEGA
卷 6, 期 8, 页码 5244-5254出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsomega.0c05263
关键词
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资金
- Science & Technology Development Fund in Egypt STDF [22909]
- Taif University, Taif, Saudi Arabia [TURSP-2020/05]
A series of new metal complexes were synthesized and tested for their anti-tumor activities on colorectal carcinoma cells and normal cells. Most of the compounds showed significant inhibitory effects on cancer cells while having no impact on normal cells.
Several metal complexes of methyl-3-(4-chlorophenyl)-3-hydroxy-2,2-dimethylpropanoate derivatives were synthesized and tested for their anti-tumor activities. The ligands include 3-(4-chlorophenyl)-3-hydroxy-2,2-dimethylpropanoic acid (1), 3-(4-chlorophenyl)-3-hydroxy-2,2-dimethylpropanehydrazide (2), and 3-(4-chlorophenyl)-N'-(4-(dimethylamino)benzylidene)-3-hydroxy-2,2-dimethylpropanehydrazide (3). The ligands were reacted with Cu (II), Ni (II), and La (III) ions. The formed complexes were characterized using elemental analysis (M%), molar conductivity in DMF (0.001 M), DTA, TG, FTIR, ICP-AES, and magnetic susceptibility. The chemical structures of the obtained complexes were interpreted, and their chemical formulas were postulated. The anti-cancer activities of these complexes were examined on human colorectal carcinoma cells (HCT-116) and also on normal cells (HEK-293). The 48 h post treatments showed that out of 12 compounds, 10 compounds showed inhibitory actions on HCT-116 cells, whereas two compounds did not show any inhibitory actions. Compounds 6c and 4a showed the highest inhibitory actions with IC50 = 0.154 and 0.18 mM and additionally compounds 3, 4b, and 6a with IC50 = 0.267, 0.205, and 0.284 mM, respectively. All tested compounds did not show any inhibitory action on normal HEK-293 cells. Molecular docking results provided a good evidence for activity of the lead compounds 3 and 4a as CDK8-CYCC kinase inhibitors, which may proposed the mechanism of action toward colon cancer therapy.
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