Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10588198 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
4-(1,3-Benzothiazol-2-yl)thiophene-2-sulfonamide (4a) was found to be a moderately potent inhibitor of cyclin-dependent kinase 5 (cdk5) from a HTS screen. The synthesis and SAR around this hit is described. The X-ray coordinates of ligand 4a with cdk5 are also reported, showing an unusual binding mode to the hinge region via a water molecule.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jonas Malmström, Jenny Viklund, Can Slivo, Ana Costa, Mickaël Maudet, Catrin Sandelin, Gösta Hiller, Lise-Lotte Olsson, Anna Aagaard, Stefan Geschwindner, Yafeng Xue, Mervi Vasänge,