The hit-to-lead optimization of 1,2,3,4,4a,9a-hexahydro-1H-xanthenes as glucocorticoid receptor antagonists
文献类型：期刊论文
| 作者 | Zhu, Yan-Hui2; Zhang, Meng2; Li, Qun-Yi2; Liu, Qing1,2; Zhang, Jie2; Yuan, Yun-Yun2; Nan, Fa-Jun1,2 ; Wang, Ming-Wei1,2
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| 刊名 | CHINESE CHEMICAL LETTERS
 |
| 出版日期 | 2014-05 |
| 卷号 | 25期号:5页码:693-698 |
| 关键词 | Glucocorticoid receptor Antagonist 1,2,3,4,4a,9a-Hexahydroxanthene Structure-activity relationship Lead optimization |
| ISSN号 | 1001-8417 |
| DOI | 10.1016/j.cc1et.2014.03.017 |
| 文献子类 | Article |
| 英文摘要 | The structure activity relationship (SAR) study of a 1,2,3,4,4a,9a-hexahydro-1H-xanthene series of selective, human glucocorticoid receptor alpha (hGR alpha) antagonists is reported. Compounds were screened using hydroxyapatite-based GR binding and MMTV-Luc co-transfection reporter gene assays. Four different regions of the scaffold were modified to assess the effects on hGRa antagonism and related potency. Compound 8d exhibits an 8-fold better bioactivity than the original hit 1a, as well as an improved chemical stability, which make it a promising lead for the subsequent optimization. (C) 2014 Ming-Wei Wang. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved. |
| WOS关键词 | SUBSTITUTED SALICYLALDEHYDES ; DERIVATIVES ; MICE |
| 资助项目 | Ministry of Health of China[2012ZX09304-011] ; Ministry of Health of China[2013ZX09401003-005] ; Ministry of Health of China[2013ZX09507001] ; Ministry of Health of China[2013ZX09507002] ; Shanghai Science and Technology Development Fund[13DZ2290300] ; Thousand Talents Program in China[00000000] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| CSCD记录号 | CSCD:5155472 |
| WOS记录号 | WOS:000337662000009 |
| 出版者 | ELSEVIER SCIENCE INC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277085]  |
| 专题 | 国家新药筛选中心 |
| 通讯作者 | Wang, Ming-Wei |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Medico, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Zhu, Yan-Hui,Zhang, Meng,Li, Qun-Yi,et al. The hit-to-lead optimization of 1,2,3,4,4a,9a-hexahydro-1H-xanthenes as glucocorticoid receptor antagonists[J]. CHINESE CHEMICAL LETTERS,2014,25(5):693-698. |
| APA | Zhu, Yan-Hui.,Zhang, Meng.,Li, Qun-Yi.,Liu, Qing.,Zhang, Jie.,...&Wang, Ming-Wei.(2014).The hit-to-lead optimization of 1,2,3,4,4a,9a-hexahydro-1H-xanthenes as glucocorticoid receptor antagonists.CHINESE CHEMICAL LETTERS,25(5),693-698. |
| MLA | Zhu, Yan-Hui,et al."The hit-to-lead optimization of 1,2,3,4,4a,9a-hexahydro-1H-xanthenes as glucocorticoid receptor antagonists".CHINESE CHEMICAL LETTERS 25.5(2014):693-698. |
入库方式： OAI收割
来源：上海药物研究所
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