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Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes

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Voigt, B. | Meijer, L. | Lozach, O. | Schachtele, C. | Totzke, F. | Hilgeroth, A.

Edité par CCSD ; Elsevier -

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.

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