期刊
CHEMICAL & PHARMACEUTICAL BULLETIN
卷 67, 期 7, 页码 725-728出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.c19-00217
关键词
chalcone; indole; naphthalene; tubulin; anticancer activity
资金
- National Natural Science Foundation of China [81660574]
- one thousand Talents Program of Guizhou Province (the fifth group)
- basic research plan of Guizhou province [[2019]1256]
- Doctor Foundation of Guizhou Medical University [[2018]004]
Eighteen novel chalcone derivatives containing indole and naphthalene moieties (2-19) were synthesized and characterized by H-1-NMR, C-13-NMR and high resolution (HR)-MS spectra. All compounds were evaluated for their in vitro cytotoxic potential against human hepatocellular carcinoma (HepG2), human colon carcinoma (HCT116) and human breast adenocarcinoma (MCF-7) cell lines. Among them, compound 2, 3, 4 and 7 showed potent activities against tested cancer cell lines. More significantly, compound 7 exhibited the most potent cytotoxic activity against HepG2, HCT116 and MCF-7 with IC50 values of 0.65, 1.13 and 0.82 mu M, respectively. Furthermore, flow cytometry analysis indicated that compound 7 arrested cancer cells in G2/M phase. The compound 7 also displayed significant inhibition of tubulin polymerization (IC50 = 3.9 mu M). Finally, molecular docking studies were performed to explore the possible interactions between compound 7 and tubulin binding pockets.
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