期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 61, 期 17, 页码 7785-7795出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.8b00765
关键词
-
资金
- National Institutes of Health [CA156732, HD093540-01, CA066996]
- EUNICE KENNEDY SHRIVER NATIONAL INSTITUTE OF CHILD HEALTH & HUMAN DEVELOPMENT [P50HD093540, U54HD093540] Funding Source: NIH RePORTER
- NATIONAL CANCER INSTITUTE [U54CA156732, P01CA066996] Funding Source: NIH RePORTER
The simultaneous inhibition of polo-like kinase 1 (PLK1) and BRD4 bromodomain by a single molecule could lead to the development of an effective therapeutic strategy for a variety of diseases in which PLK1 and BRD4 are implicated. Compound 23 has been found to be a potent dual kinase-bromodomain inhibitor (BRD4-BD1 IC50 = 28 nM, PLK1 IC 50 = 40 nM). Compound 6 was found to be the most selective PLK1 inhibitor over BRD4 in our series (BRD4-BD1 IC50 = 2579 nM, PLK1 IC50 = 9.9 nM). Molecular docking studies with 23 and BRD4-BD1/PLK1 as well as with 6 corroborate the biochemical assay results.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据