Design and synthesis of pregnenolone/2-cyanoacryloyl conjugates with dual NF-kappa B inhibitory and anti-proliferative activities
文献类型：期刊论文
| 作者 | Song, Jia-Li6; Zhang, Juan4,5 ; Liu, Chang-Liang3; Liu, Chao2; Zhu, Kong-Kai6; Yang, Fei-Fei6; Liu, Xi-Gong6; Longo, Joao Paulo Figueiro4,5; Muehlmann, Luis Alexandre4,5; Azevedo, Ricardo Bentes4
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2017-10-15 |
| 卷号 | 27期号:20页码:4682-4686 |
| 关键词 | Pregnenolone NF-kappa B 2-Cyanoacryloyl Michael acceptor Anti-proliferative activity |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2017.09.013 |
| 文献子类 | Article |
| 英文摘要 | Twenty-five novel pregnenolone/2-cyanoacryloyl conjugates (6-30) were designed and prepared, with the aim of developing novel anticancer drugs with dual NF-kappa B inhibitory and anti-proliferative activities. Compounds 22 and 27-30 showed inhibition against TNF-alpha-induced NF-kappa B activation in luciferase assay, which was confirmed by Western blotting. Among them, compound 30 showed potent NF-kappa B inhibitory activity (IC50 = 2.5 mu M) and anti-proliferative against MCF-7, A549, H157, and HL-60 cell lines (IC50 = 6.5-36.2 mu M). The present study indicated that pregnenolone/2-cyanoacryloyl conjugate I can server as a novel scaffold for developing NF-kappa B inhibitors and anti-proliferative agents in cancer chemotherapy. (C) 2017 Elsevier Ltd. All rights reserved. |
| WOS关键词 | BIOLOGICAL EVALUATION ; AGENTS ; PREGNENOLONE ; DERIVATIVES ; TOXICITY ; UPDATE ; TARGET ; CELLS |
| 资助项目 | Natural Science Foundation of China[21672082] ; Shandong Key Development Project[2016GSF201209] ; Young Taishan Scholars Program[tsqn20161037] ; Shandong Talents Team Cultivation Plan of University Preponderant Discipline[10027] ; Natural Science Foundation of Shandong Province[BS2015YY021] ; Natural Science Foundation of Shandong Province[ZR2016HB43] ; FAP/DF[00000000] ; CNPq[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000412863700017 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272446]  |
| 专题 | 天然药物化学研究室 |
| 通讯作者 | Zhang, Yu-Ying; Jiang, Cheng-Shi; Zhang, Hua |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 2.Shandong Acad Agr Sci, Inst Agrofood Sci & Technol, Jinan 250100, Shandong, Peoples R China; 3.Harvard Med Sch, Dept Neurobiol, Boston, MA 02115 USA; 4.Univ Brasilia, Inst Biol Sci, BR-70910900 Brasilia, DF, Brazil; 5.Univ Brasilia, Fac Ceilandia, BR-72220275 Brasilia, DF, Brazil; 6.Univ Jinan, Sch Biol Sci & Technol, Jinan 250022, Shandong, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Song, Jia-Li,Zhang, Juan,Liu, Chang-Liang,et al. Design and synthesis of pregnenolone/2-cyanoacryloyl conjugates with dual NF-kappa B inhibitory and anti-proliferative activities[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2017,27(20):4682-4686. |
| APA | Song, Jia-Li.,Zhang, Juan.,Liu, Chang-Liang.,Liu, Chao.,Zhu, Kong-Kai.,...&Zhang, Hua.(2017).Design and synthesis of pregnenolone/2-cyanoacryloyl conjugates with dual NF-kappa B inhibitory and anti-proliferative activities.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,27(20),4682-4686. |
| MLA | Song, Jia-Li,et al."Design and synthesis of pregnenolone/2-cyanoacryloyl conjugates with dual NF-kappa B inhibitory and anti-proliferative activities".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 27.20(2017):4682-4686. |
入库方式： OAI收割
来源：上海药物研究所
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