Synthesis and Anti-tumor Activity of Novel Garcinol Analogs

被引：1
|
作者：
Zhou, Huiyuan [1 ]
Wu, Yanlin [2 ]
Huang, Dianhong [1 ]
Zhang, Mingting [1 ]
Chen, Huanming [1 ]
Qian, Mingcheng [1 ]
Zhao, Shuai [1 ]
Zhang, Xinyan [2 ]
Chen, Xin [1 ]
机构：
[1] Changzhou Univ, Sch Pharmaceut Engn & Life Sci, Changzhou 213164, Jiangsu, Peoples R China
[2] Capital Med Univ, Beijing Stomatol Hosp, Beijing Inst Dent Res, Beijing 100050, Peoples R China
来源：
CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2020年 / 40卷 / 06期
基金：
中国国家自然科学基金;
关键词：
garcinol; structural modification; Michael addition; anti-tumor; ANTICANCER; SUPPRESSION; MRSA;
D O I：
10.6023/cjoc202001016
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
Garcinol possesses a wide range of biological activities, such as anti-inflanunation, anti-tumors, anti-oxidation, induction of apoptosis and so on. In this paper, the modification of the side chains in garcinol was carried out to enhance its anti-tumor activity. Employing acetylacetone as starting material , three new analogs of garcinol were prepared by means of Michael addition, Knoevenagel condensation, and so on. Furthemore, their biological activity was assessed by methyl thiazolvl tetrazolium (MTT) method and the structure-activity relationship was analyzed. The results showed that the inhibitory activities of the three new analogs on oral squamous cell carcinoma were moderately lower than that of garcinol. Hence, the isoprenyl group at the C4 position and the allylic group at the C8 position might play vital roles for the biological activity of garcinol.
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收藏
页码：1578 / 1587
页数：10
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