Design,Synthesis and Anticancer Activity of Shikonin and Alkannin Derivatives with Different Substituents on the Naphthazarin Scaffold |
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Authors: | ZHANG Xu CUI Jiahua ZHOU Wen LI Shaoshun |
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Affiliation: | School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, P. R. China |
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Abstract: | Based on the asymmetric reduction of alkannin ketone derivative 4 by diisopinocampheylchloro-borane(DIP-Cl), a series of shikonin and alkannin derivatives was designed, synthesized and their anticancer activities against various kinds of cell lines were evaluated. The in vitro biological experiments demonstrated that compound S-10, a 5,8-O-dimethyl-1,4-dioxime alkannin derivative, not only displayed excellent antiproliferative activity against cancer cells, but also exhibited low toxicity towards normal cells. It could induce HCT-116 cell apoptosis, but had no impact on the cell cycle. The underlying anticancer mechanism of S-10 is most likely different from other shikonin and alkannin derivatives. |
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Keywords: | Shikonin and alkannin oxime derivative Asymmetric reduction Anticancer Apoptosis Cell cycle |
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