Novel aspects in structure–activity relationships of profiled 1-aza-9-oxafluorenes as inhibitors of Alzheimer's disease-relevant kinases cdk1, cdk5 and gsk3β
Volkmar Tell, Kazem Mahmoud, Kanin Wichapong, Christoph Schächtele, Frank Totzke, Wolfgang Sippl, Andreas Hilgeroth · MedChemComm · 2012
A novel series of derivatized 1-aza-9-oxafluorenes has been synthesized. Structure-directed substituents have been introduced and their effect on the inhibition of Alzheimer's disease-relevant kinases has been determined in in vitro assays. Novel structure–activity relationships were found depending on the varying substituents. Nanomolar inhibitors have been identified as promising candidates for the treatment of Alzheimer's disease.