期刊
MEDICINAL CHEMISTRY RESEARCH
卷 26, 期 9, 页码 1871-1883出版社
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-017-1891-0
关键词
Chalcone; alpha,beta-Unsaturated; Carbonyl; Anticervical cancer molecular modeling; Anti-mitotic; Synthesis
资金
- Natural National Science Foundation of China [81260379]
A series of 31 chalcones were synthesized and evaluated for anti-proliferative activity against the human cervical cancer cell lines (HeLa and SiHa). Compound 19, (E)-1-(2,4-dihydroxyphenyl)-3-(4-(dimethylamino)phenyl)-2-methylprop-2-en-1-one was found to be an effective anti-proliferative agent in HeLa and SiHa cells (IC50 = 0.035 mu M). Compound 19 increased the percentage of apoptosis in a dose-dependent manner, as measured by Annexin V-FITC (fluorescein isothiocyanate)/(propidium iodide) PI staining. Molecular modeling studies of compound 19 showed that the most potent structure was docked at the yeast 20 S proteasome binding site (Protein Data Bank code-3E47) and was stabilized in the cavity by various hydrophobic and hydrogen bonding interactions.
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