thehittoleadoptimizationof12344a9ahexahydro1hxanthenesasglucocorticoidreceptorantagonists
文献类型：期刊论文
| 作者 | Zhu Yanhui; Zhang Meng; Li Qunyi; Liu Qing; Zhang Jie; Yuan Yunyun; Nan Fajun ; Wang Mingwei
|
| 刊名 | chinesechemicalletters
 |
| 出版日期 | 2014 |
| 卷号 | 25期号:5页码:693 |
| 关键词 | SUBSTITUTED SALICYLALDEHYDES DERIVATIVES MICE 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 |
| 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. |
| 资助项目 | [Ministry of Health of China] ; [Shanghai Science and Technology Development Fund] ; [Thousand Talents Program in China] |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/286672]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | Zhu Yanhui,Zhang Meng,Li Qunyi,et al. thehittoleadoptimizationof12344a9ahexahydro1hxanthenesasglucocorticoidreceptorantagonists[J]. chinesechemicalletters,2014,25(5):693. |
| APA | Zhu Yanhui.,Zhang Meng.,Li Qunyi.,Liu Qing.,Zhang Jie.,...&Wang Mingwei.(2014).thehittoleadoptimizationof12344a9ahexahydro1hxanthenesasglucocorticoidreceptorantagonists.chinesechemicalletters,25(5),693. |
| MLA | Zhu Yanhui,et al."thehittoleadoptimizationof12344a9ahexahydro1hxanthenesasglucocorticoidreceptorantagonists".chinesechemicalletters 25.5(2014):693. |
入库方式： OAI收割
来源：上海药物研究所
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