Synthesis and biological activity of some antitumor active derivatives from glycyrrhetinic acid

René Csuk; Stefan Schwarz; Ralph Kluge; Dieter Ströhl

doi:10.1016/j.ejmech.2010.09.028

Synthesis and biological activity of some antitumor active derivatives from glycyrrhetinic acid

Eur J Med Chem. 2010 Dec;45(12):5718-23. doi: 10.1016/j.ejmech.2010.09.028. Epub 2010 Sep 17.

Authors

René Csuk¹, Stefan Schwarz, Ralph Kluge, Dieter Ströhl

Affiliation

¹ Bereich Organische Chemie, Martin-Luther-Universität Halle-Wittenberg, Kurt-Mothes-Str. 2, D-06120 Halle, Saale, Germany. rene.csuk@chemie.uni-halle.de

PMID: 20884085
DOI: 10.1016/j.ejmech.2010.09.028

Abstract

Aminoalkyl substituted derivatives were synthesized starting from glycyrrhetinic acid methyl ester and screened for antitumor activity in a panel of 15 human cancer cell lines by an SRB assay. The most compound 7 possesses an aminohexyl side chain, induces apoptosis and shows IC50 values of 0.6-3.0 μM.

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Apoptosis / drug effects
Cell Proliferation / drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Glycyrrhetinic Acid / chemical synthesis
Glycyrrhetinic Acid / chemistry
Glycyrrhetinic Acid / pharmacology*
Humans
Molecular Conformation
Stereoisomerism
Structure-Activity Relationship
Tumor Cells, Cultured

Substances

Antineoplastic Agents
Glycyrrhetinic Acid