Approaches to a Multitargeting Drug Development: First Profiled 3- Ethoxycarbonyl-1-aza-9-oxafluorenes Representing a Perspective Compound Class Targeting Alzheimer Disease Relevant Kinases CDK1, CDK5 and GSK-3β

Author(s): Andreas Hilgeroth, Volkmar Tell, Steffi Kramer, Frank Totzke, Christoph Schachtele

Journal Name: Medicinal Chemistry

Volume 10 , Issue 1 , 2014

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Since Alzheimer disease (AD) is a multifactorial disease, recent therapeutical approaches concentrate on the development of a multitargeting drug. Various protein kinases are known to be involved in the progression of AD. A first series of 3-ethoxycarbonyl-1-aza-9-oxafluorenes has been synthesized and biologically evaluated as AD-relevant protein kinase inhibitors. A concentration-dependent inhibition of important AD-relevant kinases has been characterized after the selectivity of kinase inhibition had been demonstrated. Structure-activity relationships of protein kinase inhibition are discussed and first multitargeting inhibitors have been identified.

Keywords: Multitargeting, structure-activity relationships, biological activity, alzheimer disease, compound profiling, protein kinases.

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Article Details

Year: 2014
Published on: 26 December, 2013
Page: [90 - 97]
Pages: 8
DOI: 10.2174/157340641001131226141606

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PDF: 51