Abstract
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.
Medicinal Chemistry
Title: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
Volume: 10 Issue: 1
Author(s): Andreas Hilgeroth, Volkmar Tell, Steffi Kramer, Frank Totzke and Christoph Schachtele
Affiliation:
Keywords: Multitargeting, structure-activity relationships, biological activity, alzheimer disease, compound profiling, protein kinases.
Abstract: 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.
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Hilgeroth Andreas, Tell Volkmar, Kramer Steffi, Totzke Frank and Schachtele Christoph, 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 , Medicinal Chemistry 2014; 10 (1) . https://dx.doi.org/10.2174/157340641001131226141606
DOI https://dx.doi.org/10.2174/157340641001131226141606 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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