Please use this identifier to cite or link to this item: http://dx.doi.org/10.25673/85360
Title: Rhodamine 101 conjugates of triterpenoic amides are of comparable cytotoxicity as their Rhodamine B analogs
Author(s): Heise, Niels V.
Major, Daniel
Hoenke, Sophie
Kozubek, Marie
Serbian, Immo
Csuk, René
Issue Date: 2022
Type: Article
Language: English
Abstract: Pentacyclic triterpenoic acids (betulinic, oleanolic, ursolic, and platanic acid) were selected and subjected to acetylation followed by the formation of amides derived from either piperazine or homopiperazine. These amides were coupled with either rhodamine B or rhodamine 101. All of these compounds were screened for their cytotoxic activity in SRB assays. As a result, the cytotoxicity of the parent acids was low but increased slightly upon their acetylation while a significant increase in cytotoxicity was observed for piperazinyl and homopiperazinyl amides. A tremendous improvement in cytotoxicity was observed; however, for the rhodamine B and rhodamine 101 conjugates, and compound 27, an ursolic acid derived homopiperazinyl amide holding a rhodamine 101 residue showed an EC50 = 0.05 µM for A2780 ovarian cancer cells while being less cytotoxic for non-malignant fibroblasts. To date, the rhodamine 101 derivatives presented here are the first examples of triterpene derivatives holding a rhodamine residue different from rhodamine B.
URI: https://opendata.uni-halle.de//handle/1981185920/87312
http://dx.doi.org/10.25673/85360
Open Access: Open access publication
License: (CC BY 4.0) Creative Commons Attribution 4.0(CC BY 4.0) Creative Commons Attribution 4.0
Sponsor/Funder: Publikationsfonds MLU
Journal Title: Molecules
Publisher: MDPI
Publisher Place: Basel
Volume: 27
Issue: 7
Original Publication: 10.3390/molecules27072220
Appears in Collections:Open Access Publikationen der MLU

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