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Bioorg Med Chem Lett
; 22(18): 5919-23, 2012 Sep 15.
Article
in English
| MEDLINE
| ID: mdl-22889803
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.