Structure–activity relationship study of 2,4-diaminothiazoles as Cdk5/p25 kinase inhibitors

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dc.contributor.authorLaha, Joydev K.
dc.contributor.authorZhang, Xuemei
dc.contributor.authorQiao, Lixin
dc.contributor.authorChatterjee, Snigdha
dc.contributor.authorRobinson, Shaughnessy
dc.contributor.authorKosik, Kenneth S.
dc.contributor.authorCuny, Gregory D.
dc.date.accessioned2020-03-10T17:31:37Z
dc.date.available2020-03-10T17:31:37Z
dc.date.issued2012-04
dc.description.abstractCdk5/p25 has emerged as a principle therapeutic target for numerous acute and chronic neurodegenerative diseases, including Alzheimer’s disease. A structure–activity relationship study of 2,4-diaminothiazole inhibitors revealed that increased Cdk5/p25 inhibitory activity could be accomplished by incorporating pyridines on the 2-amino group and addition of substituents to the 2- or 3-position of the phenyl ketone moiety. Interpretation of the SAR results for many of the analogs was aided through in silico docking with Cdk5/p25 and calculating protein hydrations sites using WaterMap. Finally, improved in vitro mouse microsomal stability was also achieved.
dc.identifier.citationCopyright 2011 Bioorganic and Medicinal Chemistry Letters. This is a post-print version of a published paper that is available at: https://www.sciencedirect.com/science/article/pii/S0960894X11001740. Recommended citation: Laha, Joydev K., Xuemei Zhang, Lixin Qiao, Min Liu, Snigdha Chatterjee, Shaughnessy Robinson, Kenneth S. Kosik, and Gregory D. Cuny. "Structure–activity relationship study of 2, 4-diaminothiazoles as Cdk5/p25 kinase inhibitors." Bioorganic & medicinal chemistry letters 21, no. 7 (2011): 2098-2101. doi: 10.1016/j.bmcl.2011.01.140. This item has been deposited in accordance with publisher copyright and licensing terms and with the author's permission.
dc.identifier.urihttps://hdl.handle.net/10657/5959
dc.language.isoen_US
dc.publisherBioorganic and Medicinal Chemistry Letters
dc.subjectCdk5
dc.subjectKinase
dc.subjectInhibitor
dc.subjectAlzheimer's disease
dc.subject2,4-diaminothiazoles
dc.titleStructure–activity relationship study of 2,4-diaminothiazoles as Cdk5/p25 kinase inhibitors
dc.typeArticle

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