Synthesis and biological activity of some antitumor active derivatives from glycyrrhetinic acid.
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.
Csuk
René
R
Bereich Organische Chemie, Martin-Luther-Universität Halle-Wittenberg, Kurt-Mothes-Str. 2, D-06120 Halle, Saale, Germany. rene.csuk@chemie.uni-halle.de
Schwarz
Stefan
S
Kluge
Ralph
R
Ströhl
Dieter
D
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006034:Glycyrrhetinic Acid / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008968:Molecular Conformation; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D006034:Glycyrrhetinic Acid