Design and synthesis of oridonin derivatives as cytotoxic agents

被引：1

作者：

Zhao, Chen-Liang ^{[1
,2
]}

Zhang, Chi-Yuan ^{[1
]}

Yang, Xiao-Min ^{[1
]}

Xia, Yi-Xuan ^{[1
]}

Du, Yin-Xiao ^{[1
]}

Pan, Lu-Tai ^{[2
]}

Lam, Ka Hei ^{[1
]}

Zhang, Hong-Jie ^{[1
]}

机构：

[1] Hong Kong Baptist Univ, Sch Chinese Med, Hong Kong, Peoples R China

[2] Guizhou Univ Tradit Chinese Med, Guiyang 550025, Peoples R China

来源：

NATURAL PRODUCT RESEARCH | 2025年 / 39卷 / 03期

关键词：

Oridonin; anticancer; ent-kaurane diterpenoid; derivatives; cytotoxicity; PROTEIN; DRUGS;

D O I：

10.1080/14786419.2023.2275287

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Oridonin is one of the ent-kaurane diterpenes that have been studied extensively for various bioactivities. In an effort to expand natural scaffold-based library as anticancer agents, we have designed and synthesised a number of novel oridonin derivatives and evaluated their bioactivities on a panel of human cancer cell lines (HCT116, A375, MCF-7, HepG2, and A549). Compound 4b bearing a 4-fluorophenyl moiety was found to be the most active compound with an IC50 value of 0.3 mu M against MCF-7 cells, which was 7.4-fold more active than oridonin. This study could provide some insightful information for further synthesis of oridonin derivatives as anticancer agents.

引用

页码：550 / 558

页数：9

共 16 条

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