<sup>1</sup>H and <sup>13</sup>C NMR spectral assignments of flavone derivatives

Kim, Beom Soo; Koh, Eun Jee; Jung, Yearam; Shin, Soon Young; Lim, Yoongho

doi:10.1002/mrc.4535

Cited by 2 publications

(2 citation statements)

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“…The synthesis and identification of flavone derivatives containing hydroxy, fluoro, bromo, nitro, methoxy, methyl, styryl, and/or naphthalenyl groups were reported previously [7]. The synthetic scheme is provided as Scheme S1 [7]. The names of the derivatives are listed in Table 1.…”

Section: Methodsmentioning

confidence: 99%

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Inhibitory Effect of Synthetic Flavone Derivatives on Pan-Aurora Kinases: Induction of G2/M Cell-Cycle Arrest and Apoptosis in HCT116 Human Colon Cancer Cells

Shin

Lee

Kim

et al. 2018

IJMS

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Members of the aurora kinase family are Ser/Thr kinases involved in regulating mitosis. Multiple promising clinical trials to target aurora kinases are in development. To discover flavones showing growth inhibitory effects on cancer cells, 36 flavone derivatives were prepared, and their cytotoxicity was measured using a long-term clonogenic survival assay. Their half-maximal growth inhibitory effects against HCT116 human colon cancer cells were observed at the sub-micromolar level. Pharmacophores were derived based on three-dimensional quantitative structure–activity calculations. Because plant-derived flavones inhibit aurora kinase B, we selected 5-methoxy-2-(2-methoxynaphthalen-1-yl)-4H-chromen-4-one (derivative 31), which showed the best half-maximal cell growth inhibitory effect, and tested whether it can inhibit aurora kinases in HCT116 colon cancer cells. We found that derivative 31 inhibited the phosphorylation of aurora kinases A, aurora kinases B and aurora kinases C, suggesting that derivative 31 is a potential pan-aurora kinase inhibitor. The results of our analysis of the binding modes between derivative 31 and aurora A and aurora B kinases using in-silico docking were consistent with the pharmacophores proposed in this study.

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Section: Methodsmentioning

confidence: 99%

“…In order to identify the structural characteristics of flavones exhibiting growth inhibitory effects on cancer cells, we prepared 36 synthetic flavone derivatives containing hydroxy, fluoro, bromo, nitro, methoxy, methyl, styryl or naphthalenyl groups [7]. Colon cancer is the second most diagnosed cancer in women and the third in men [8].…”

Section: Introductionmentioning

confidence: 99%