| Literature DB >> 21742493 |
Yonghan Hu1, Derek Cole, Rajiah Aldrin Denny, David R Anderson, Manus Ipek, Yike Ni, Xiaolun Wang, Suvit Thaisrivongs, Timothy Chamberlain, J Perry Hall, Julie Liu, Michael Luong, Lih-Ling Lin, Jean-Baptiste Telliez, Ariamala Gopalsamy.
Abstract
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.Entities:
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Year: 2011 PMID： 21742493 DOI： 10.1016/j.bmcl.2011.06.065
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823