title: Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes.
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.
authors.affiliation: Institute of Pharmaceutical Chemistry, Department of Pharmacy, Martin-Luther-University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, 06120 Halle, Germany.
authors.forename: Burkhardt
authors.initials: B
authors.lastname: Voigt
authors.forename: Laurent
authors.initials: L
authors.lastname: Meijer
authors.forename: Olivier
authors.initials: O
authors.lastname: Lozach
authors.forename: Christoph
authors.initials: C
authors.lastname: Schächtele
authors.forename: Frank
authors.initials: F
authors.lastname: Totzke
authors.forename: Andreas
authors.initials: A
authors.lastname: Hilgeroth
mesh_terms: D001665:Binding Sites; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis; D005449:Fluorenes / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D006860:Hydrogen Bonding; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D005449:Fluorenes; D018844:Cyclin-Dependent Kinases