Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)-thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors |
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| 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 |
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| Institution: | Medicinal Chemistry, CNSP iMed Science, AstraZeneca R&D, Innovative Medicines, SE-15185 S?dert?lje, Sweden. |
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| 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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