Synthesis and Anti-tumor Activity Study of Shogaol Analogues
Journal: Journal of Pharmacy and Pharmacology (Vol.6, No. 10)Publication Date: 2018-10-10
Authors : Song Lei; Duan Yu Xu Da; Mao Yu;
Page : 907-919
Keywords : ;
Abstract
As one of the largest global public health problems, cancer greatly endangers human health. Researchers have been committed to discovering anticancer drugs with high efficiency and low toxicity. Shogaol, a kind of ingredient from ginger with high anti-tumor activity, has attracted our attention. This study was an investigation on the composition and structure-activity relationship of different analogues of shogaol, with the purpose to screen for shogaol compounds which had higher anti-tumor activity and could be easily synthesized. We chose zingerone as the starting material to synthesize shogaol through four-step reactions without protective group, as a result, 31 analogues were synthesized for anti-tumor activity detect. The biological test results showed that: the missing of the unsaturated ketone and the phenolic hydroxyl group reduced the anti-tumor activity of shogaol; the site of phenolic hydroxyl had no significant influence on the anti-tumor activity, the indicating that the larger the steric hindrance of substituent, the lower the activity, but the higher the activity of cyclobutyl substituted derivatives.
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