Autor: |
Yike Ni, Derek C. Cole, Rajiah Aldrin Denny, Julie Liu, David R. Anderson, Timothy Chamberlain, Yonghan Hu, Lih-Ling Lin, Manus Ipek, J. Perry Hall, Suvit Thaisrivongs, Michael Luong, Xiaolun Wang, Jean-Baptiste Telliez, Ariamala Gopalsamy |
Rok vydání: |
2011 |
Předmět: |
|
Zdroj: |
Bioorganicmedicinal chemistry letters. 21(16) |
ISSN: |
1464-3405 |
Popis: |
Synthesis, modeling and structure–activity relationship of indazoles as inhibitors of Tpl2 kinase are described. From a high throughput screening effort, we identified an indazole hit compound 5 that has a single digit micromolar Tpl2 activity. Through SAR modifications at the C3 and C5 positions of the indazole, we discovered compound 31 with good potency in LANCE assay and cell-based p -Erk assay. |
Databáze: |
OpenAIRE |
Externí odkaz: |
|