Open AccessGlycyrrhetinic amides and their cytotoxicity
Author(s) -
Niels V. Heise,
Sophie Hoenke,
Ahmed AlHarrasi,
HansPeter Deigner,
René Csuk
Publication year - 2021
Publication title -
mediterranean journal of chemistry
Language(s) - English
Resource type - Journals
ISSN - 2028-3997
DOI - 10.13171/mjc02110161595cesuk
Subject(s) - cytotoxicity , chemistry , sulforhodamine b , ethylenediamine , stereochemistry , cytotoxic t cell , ring (chemistry) , medicinal chemistry , organic chemistry , in vitro , biochemistry
3- O -Acetyl-glycyrrhetinic amides were prepared, and sulforhodamine B assays investigated their cytotoxicity. Their cytotoxicity strongly depended on the substitution pattern of the respective compounds. Thereby, an ethylenediamine-derived compound 2 performed the best, acting mainly by apoptosis. As far as heterocyclic amides are concerned, ring enlargement and the replacement of the distal nitrogen invariably led to a more or less complete loss of cytotoxic activity. Thus, the presence of a carbonyl function (C-30) seems necessary for providing significant cytotoxicity.