Andreas Hilgeroth, Volkmar Tell, Steffi Kramer, Frank Totzke and Christoph Schachtele Pages 90 - 97 ( 8 )
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.
Multitargeting, structure-activity relationships, biological activity, alzheimer disease, compound profiling, protein kinases.
Pharmacy, Martin- Luther University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, 06120 Halle, Germany.