Abstract
A novel series of resveratrol derivatives were synthesized according to Wittig-Horner reaction with 3,5-dihydroxybenzyl alcohol or 3,5-dimethoxybenzyl alcohol or 4-hydroxybenzyl alcohol as raw material and the inhibitory activities on breast carcinoma (MDA-MB-231) and gastric carcinoma cell lines (SGC-7901) in vitro were evaluated by the standard methyl thiazole tetrazolium (MTT) method. The result of biological test shows that some of resveratrol derivatives possess stronger anti-cancer activities than 5-FU. Compound 5c shows the strongest activity against breast carcinoma (MDA-MB-231) and gastric carcinoma cell lines (SGC-7901) with IC50 value of 50.19 ± 1.02 μM, 122.68.27 ± 2.04 μM, compared to that IC50 value of 5-FU is 98.59±3.61 μM,156.74±6.16 μM, respectively.
Highlights
Cancer is the term used for diseases in which abnormal cells divide without control and are able to invade other tissues
With this concept in mind, we introduce lipophilic group to ring A or B, and alkylate the instability of the hydroxyl in order to provide lead compounds for independent innovation of anti-cancer drugs by designing and synthesizing a series of new and trifluoromethyl resveratrol derivatives and evaluating the anti-cancer to breast carcinoma (MDA-MB-231) and gastric carcinoma cell lines (SGC7901)
The in vitro anti-cancer activities of flourine-substituted resveratrol derivatives were studied on human cells breast carcinoma (MDA-MB-231) and gastric carcinoma cell lines (SGC-7901) by applying the methyl thiazole tetrazolium (MTT) assay as described by Mosmann [20]
Summary
Cancer is the term used for diseases in which abnormal cells divide without control and are able to invade other tissues. The anti-oxidative and anti-inflammatory effects of resveratrol play a critical role in the therapeutic processing, evidence has revealed that resveratrol acts as a free radical scavenger; it promotes nitric oxide production, increases HDL cholesterol, and inhibits platelet coagulation and vasodilation [15] These biological effects may explain the strange phenomenon “French paradox”, a decreased incidence of cardiovascular diseases in moderate consumers of red wines despite an intake of a high-fat diet [16]. From the structure-activity relationship of resveratrol study, it was proved that the lipophilic groups introduced in the structure help to improve the bioactivity With this concept in mind, we introduce lipophilic group to ring A or B, and alkylate the instability of the hydroxyl in order to provide lead compounds for independent innovation of anti-cancer drugs by designing and synthesizing a series of new and trifluoromethyl resveratrol derivatives and evaluating the anti-cancer to breast carcinoma (MDA-MB-231) and gastric carcinoma cell lines (SGC7901)
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