Development of actein derivatives as potent anti-triple negative breast cancer agents
文献类型：期刊论文
| 作者 | Zhang,Honglin; Chen,Yiyan; Huang,Songwen; Xiao,Wen-Wen; Qiu,Ming-Hua ; Shao,Li-Dong; Chen,Chuan-Huizi; Li,Dashan
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2023 |
| 卷号 | 89页码:129307 |
| 关键词 | Actein Modification Triple negative breast cancer Structure-activity relationships Mechanism GROWTH-INHIBITORY ACTIVITY BLACK COHOSH EXTRACTS |
| ISSN号 | 1464-3405 |
| DOI | 10.1016/j.bmcl.2023.129307 |
| 英文摘要 | 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. |
| 学科主题 | Pharmacology & Pharmacy ; Chemistry |
| WOS记录号 | WOS:000994516900001 |
| 源URL | [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. |
入库方式： OAI收割
来源：昆明植物研究所
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