Development of actein derivatives as potent anti-triple negative breast cancer agents

doi:10.1016/j.bmcl.2023.129307

KIB OpenIR

	Development of actein derivatives as potent anti-triple negative breast cancer agents
	Zhang,Honglin; Chen,Yiyan; Huang,Songwen; Xiao,Wen-Wen; Qiu,Ming-Hua; Shao,Li-Dong; Chen,Chuan-Huizi; Li,Dashan
	2023
发表期刊	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN	1464-3405
卷号	89 页码:129307
摘要	Actein is a natural triterpenoid glycoside, isolated from the rhizomes of Cimicifuga foetida, which have been demonstrated to be potential in the treatment of breast cancer previously. Herein, we described the design and synthesis of a series of actein derivatives as anti-triple negative breast cancer (TNBC) inhibitors. Of which, the most promising derivative 27 exhibited significant inhibitory activity against human TNBC cell lines HCC1806 and MDA-MB-231, with IC50 values of 2.78 and 9.11 mu M, respectively. Structure-activity relationships of actein derivatives were also discussed. Moreover, preliminary mechanism investigation revealed that 27 significantly inhibited cancer cell proliferation via cell cycle arrest at S phase. In addition, western blot analysis showed that the activation of MAPK signaling pathway might contribute to derivative 27 induced cell death. Overall, these results indicate that 27 has the potential to be developed as a lead compound and compounds with the actein scaffold are a promising novel class of inhibitors to treat TNBC.
关键词	Actein Modification Triple negative breast cancer Structure-activity relationships Mechanism GROWTH-INHIBITORY ACTIVITY BLACK COHOSH EXTRACTS
学科领域	Pharmacology & Pharmacy ; Chemistry
DOI	10.1016/j.bmcl.2023.129307
收录类别	SCI
WOS记录号	WOS:000994516900001
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/75461
专题	中国科学院昆明植物研究所
推荐引用方式 GB/T 7714	Zhang,Honglin,Chen,Yiyan,Huang,Songwen,et al. Development of actein derivatives as potent anti-triple negative breast cancer agents[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2023,89:129307.
APA	Zhang,Honglin.,Chen,Yiyan.,Huang,Songwen.,Xiao,Wen-Wen.,Qiu,Ming-Hua.,...&Li,Dashan.(2023).Development of actein derivatives as potent anti-triple negative breast cancer agents.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,89,129307.
MLA	Zhang,Honglin,et al."Development of actein derivatives as potent anti-triple negative breast cancer agents".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 89(2023):129307.

条目包含的文件		下载所有文件
文件名称/大小	文献类型	版本类型	开放类型	使用许可
1-s2.0-S0960894X2300（1187KB）	期刊论文	出版稿	开放获取	CC BY-NC-SA	浏览下载