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

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.

Cite this article as:

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