摘要
A series of novel 6-(2,4-difluorophenyl)-3-phenyl-2H-benzo[e][1,3]oxazine-2,4(3H)-dione derivatives were synthesized and evaluated for their inhibitory effects on osteoclast activities by using TRAP-staining assay. Among the tested compounds, 3d and 3h exhibited more potent osteoclast-inhibitory activities than the lead compound NDMC503 (a ring-fused structure of NDMC101), as reported in our previous study. Both 3d and 3h exhibited two-fold increase in activity compared to NDMC503. In addition, our biological results indicated that 3d and 3h could suppress RANKL-induced osteoclastogenesis-related marker genes, such as NFATc1, c-fos, TRAP, and cathepsin K. Notably, 3d could significantly attenuate the bone-resorbing activity of osteoclasts in the pit formation assay. Thus, this study might provide a new class of lead structures that warrant further development as potential anti-resorptive agents.
原文 | 英語 |
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頁(從 - 到) | 4522-4532 |
頁數 | 11 |
期刊 | Bioorganic and Medicinal Chemistry |
卷 | 23 |
發行號 | 15 |
DOIs | |
出版狀態 | 已發佈 - 7月 23 2015 |
ASJC Scopus subject areas
- 生物化學
- 分子醫學
- 分子生物學
- 藥學科學
- 藥物發現
- 臨床生物化學
- 有機化學
指紋
深入研究「Novel inhibitors of RANKL-induced osteoclastogenesis: Design, synthesis, and biological evaluation of 6-(2,4-difluorophenyl)-3-phenyl-2H-benzo[e][1,3]oxazine-2,4(3H)-diones」主題。共同形成了獨特的指紋。資料集
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CCDC 1417633: Experimental Crystal Structure Determination
Lee, C. (Contributor), Liu, F. (Contributor), Chen, C. (Contributor), Chen, T. (Contributor), Liu, F. (Contributor), Ali, A. A. A. (Contributor), Chang, D. (Contributor) & Huang, H. (Contributor), Unknown Publisher, 7月 23 2015
DOI: 10.5517/cc1jl53d, http://www.ccdc.cam.ac.uk/services/structure_request?id=doi:10.5517/cc1jl53d&sid=DataCite
資料集: Dataset