Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer
文献类型：期刊论文
| 作者 | Haiying Chen4; Jingan Huang2; Haijun Chen2; Yuqi Lin2; Suling Liu1,3; Jia Zhou4; Yingying Zhang2; Yu Gao2; Ceshi Chen5; Zheng Zheng2 |
| 刊名 | European Journal of Medicinal Chemistry
 |
| 出版日期 | 2018 |
| 期号 | 146页码:354-367 |
| 关键词 | Triple-negative Breast Cancer Mifepristone Derivatives Sensitive Metabolic Region Klf5 Expression |
| DOI | 10.1016/j.ejmech.2018.01.056 |
| 英文摘要 | Triple-negative breast cancer (TNBC) is one of the most malignant breast cancers currently with a lack oftargeted therapeutic drugs. Accumulating evidence supports that KLF5 represents a novel therapeutictarget for the treatment of basal TNBC. Our previous studies revealed that mifepristone is capable ofsuppressing TNBC cell proliferation and promoting cancer cell apoptosis by inhibiting KLF5 expression.Nevertheless, its anticancer efficacy is only modest with high dose. Moreover, its main metabolite N-desmethyl mifepristone with the removal of one methyl moiety results in a significant loss of anti-proliferative activity, indicating an important pharmacophore domain around this methyl moiety. Toimprove the pharmacokinetic properties including metabolic stability and enhance the anticancer ac-tivities, a focused compound library by altering this sensitive metabolic region of mifepristone has beendesigned and synthesized for scaffold repurposing and structural optimization. Compound 17 (FZU-00,004) has been identified with an attractive anticancer profile against TNBC via suppressing KLF5expression. |
| 语种 | 英语 |
| 源URL | [http://159.226.149.26:8080/handle/152453/12296]  |
| 专题 | 昆明动物研究所_肿瘤生物学 |
| 通讯作者 | Haijun Chen; Ceshi Chen; Ping Zhao |
| 作者单位 | 1.Institutes of Biomedical Sciences, Fudan University, Shanghai 200032, China 2.College of Chemistry, Fuzhou University, Fuzhou, Fujian 350108, China 3.Key Laboratory of Breast Cancer in Shanghai, Cancer Institute, Department of Breast Surgery, Fudan University Shanghai Cancer Center, Shanghai 200032, China 4.Chemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States 5.Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences and Yunnan Province, Chinese Academy of Sciences, Kunming Institute of Zoology, Kunming, Yunnan 650223, China |
| 推荐引用方式 GB/T 7714 | Haiying Chen,Jingan Huang,Haijun Chen,et al. Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer[J]. European Journal of Medicinal Chemistry,2018(146):354-367. |
| APA | Haiying Chen.,Jingan Huang.,Haijun Chen.,Yuqi Lin.,Suling Liu.,...&Ping Zhao.(2018).Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer.European Journal of Medicinal Chemistry(146),354-367. |
| MLA | Haiying Chen,et al."Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer".European Journal of Medicinal Chemistry .146(2018):354-367. |
入库方式： OAI收割
来源：昆明动物研究所
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