Author/Authors :
Burkhardt Voigt، نويسنده , , Laurent Meijer، نويسنده , , Olivier Lozach، نويسنده , , Christoph Sch?chtele، نويسنده , , Frank Totzke، نويسنده , , Andreas Hilgeroth، نويسنده ,
Abstract :
A series of 1-aza-9-oxafluorenes with functionally varied 3-substituents have been prepared from N-phenoxycarbonyl-4-phenyl-1,4-dihydropyridines and p-benzoquinone and biologically evaluated as inhibitors of various cyclin-dependant kinases. The absence of a 3-hydrogen bond acceptor function leads to a complete loss of inhibitory activity. Differing hydrogen bond acceptor functions surprisingly cause significant shifts in the selectivity of inhibition profiles.