3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-β.
| Autor: | Miller DD; GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK., Bamborough P, Christopher JA, Baldwin IR, Champigny AC, Cutler GJ, Kerns JK, Longstaff T, Mellor GW, Morey JV, Morse MA, Nie H, Rumsey WL, Taggart JJ |
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| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Apr 15; Vol. 21 (8), pp. 2255-8. Date of Electronic Publication: 2011 Mar 01. |
| DOI: | 10.1016/j.bmcl.2011.02.107 |
| Abstrakt: | The discovery and hit-to-lead exploration of a novel series of selective IKK-β kinase inhibitors is described. The initial lead fragment 3 was identified by pharmacophore-directed virtual screening. Homology model-driven SAR exploration of the template led to potent inhibitors, such as 12, which demonstrate efficacy in cellular assays and possess encouraging developability profiles. (Copyright © 2011 Elsevier Ltd. All rights reserved.) |
| Databáze: | MEDLINE |
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