Rhodamine B conjugates of triterpenoic acids are cytotoxic mitocans even at nanomolar concentrations.
Basic Information
ID: ALA3997779
Journal: Eur J Med Chem
Title: Rhodamine B conjugates of triterpenoic acids are cytotoxic mitocans even at nanomolar concentrations.
Authors: Sommerwerk S, Heller L, Kerzig C, Kramell AE, Csuk R.
Abstract: Triterpenoic acids 1-6 exhibited very low or no cytotoxicity at all, but their corresponding 2,3-di-O-acetyl-piperazinyl amides 13-18 showed low EC50 values for several human tumor cell lines. Their cytotoxicity, however, was also high for the non-malignant mouse fibroblasts NIH 3T3. A significant improvement was achieved by preparing the rhodamine B derivatives 19-24. While rhodamine B is not cytotoxic (up to a concentration of 30μM - cut-off of the assay), the triterpenoid piperazine-spacered rhodamine B derivatives were cytotoxic in nano-molar concentration. Compound 24 (a diacetylated maslinic acid derivative) was most toxic for several human tumor cell lines but less toxic for mouse fibroblasts NIH 3T3. Staining and double-staining experiments revealed 24 to act as a mitocan.
CiteXplore: 28033541
DOI: 10.1016/j.ejmech.2016.12.040
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