2. Academic Validation
  3. Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties

Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties

  • J Med Chem. 2003 Feb 27;46(5):876-9. doi: 10.1021/jm021090g.
Kristin Brachwitz 1,  Burkhardt Voigt,  Laurent Meijer,  Olivier Lozach,  Christoph Schächtele,  Josef Molnár,  Andreas Hilgeroth
Affiliations

Affiliation

  • 1 Institute of Pharmaceutical Chemistry, Martin-Luther-University Halle-Wittenberg, Wolfgang-Langenbeck-Strasse 4, 06120 Halle, Germany.
PMID: 12593668 DOI: 10.1021/jm021090g
Abstract

The first series of synthetic 1-aza-9-oxafluorenes with cytostatic activities in the micromolar range was evaluated as cyclin-dependent kinase (CDK1) inhibitors. Activity was found to be selective in comparison to the inhibition of Other kinases within the CDK family. Compounds were shown to inhibit the membrane-efflux pump P-glycoprotein responsible for multidrug resistance in Cancer cells. First structure-activity relationships are discussed.

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