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

Kristin Brachwitz, Burkhardt Voigt, Laurent Meijer, Olivier Lozach, Christoph Schächtele, Josef Molnár, Andreas Hilgeroth

Research output: Contribution to journalArticle

24 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)876-879
Number of pages4
JournalJournal of Medicinal Chemistry
Volume46
Issue number5
DOIs
Publication statusPublished - Feb 27 2003

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Fingerprint Dive into the research topics of 'Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties'. Together they form a unique fingerprint.

  • Cite this