Novel insight in structure-activity relationship and bioanalysis of P-glycoprotein targeting highly potent tetrakishydroxymethyl substituted 3,9-diazatetraasteranes

Claudius Coburger, Jörg Wollmann, Christiane Baumert, Martin Krug, J. Molnár, Hermann Lage, Andreas Hilgeroth

Research output: Contribution to journalArticle

20 Citations (Scopus)

Abstract

Novel 3,9-diazatetraasteranes have been synthesized with varied aromatic substitution patterns and evaluated as P-glycoprotein (P-gp) inhibitors. Structure-activity relationships (SAR) are discussed in relation to determined physicochemical properties. The potential to induce P-gp expression has been evaluated in cancer cell lines. The bioanalytical results indicate favorable noninducing properties compared to P-gp inducing drug standard.

Original languageEnglish
Pages (from-to)5871-5874
Number of pages4
JournalJournal of Medicinal Chemistry
Volume51
Issue number18
DOIs
Publication statusPublished - Sep 25 2008

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P-Glycoprotein
Structure-Activity Relationship
Cell Line
Pharmaceutical Preparations
Neoplasms

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Novel insight in structure-activity relationship and bioanalysis of P-glycoprotein targeting highly potent tetrakishydroxymethyl substituted 3,9-diazatetraasteranes. / Coburger, Claudius; Wollmann, Jörg; Baumert, Christiane; Krug, Martin; Molnár, J.; Lage, Hermann; Hilgeroth, Andreas.

In: Journal of Medicinal Chemistry, Vol. 51, No. 18, 25.09.2008, p. 5871-5874.

Research output: Contribution to journalArticle

Coburger, Claudius ; Wollmann, Jörg ; Baumert, Christiane ; Krug, Martin ; Molnár, J. ; Lage, Hermann ; Hilgeroth, Andreas. / Novel insight in structure-activity relationship and bioanalysis of P-glycoprotein targeting highly potent tetrakishydroxymethyl substituted 3,9-diazatetraasteranes. In: Journal of Medicinal Chemistry. 2008 ; Vol. 51, No. 18. pp. 5871-5874.
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