Please use this identifier to cite or link to this item:
http://dx.doi.org/10.25673/86374
Title: | Hydroxyethylamide substituted triterpenoic acids hold good cytotoxicity for human tumor cells |
Author(s): | Denner, Toni C. Hoenke, Sophie Kraft, Oliver Deigner, Hans-Peter Al-Harrasi, Ahmed Csuk, René |
Issue Date: | 2022 |
Type: | Article |
Language: | English |
Abstract: | Pentacyclic triterpenoic acids, betulinic acid, platanic acid, oleanolic acid and ursolic acid, were acetylated and subsequently converted into mono-, bis- and tris(hydroxyl)ethyl amides. While parent compounds are of none or minor cytotoxicity, these amides showed EC50 values even in low μM concentration for a variety of different human tumor cell lines. Especially a bis(hydroxyethyl)amide 12 derived from oleanolic acid held an EC50 = 7.7 μM for A375 melanoma cells while being less cytotoxic for non-malignant fibroblasts NIH 3 T3 (EC50 > 30 μM). Several of these amides were converted into their corresponding sulfamates. While these sulfamates held no inhibitory activity for the enzyme carbonic anhydrase II, the highest cytotoxicity was observed for a betulinic acid derived sulfamate 17 with an EC50 = 4.9 μM for A375 melanoma cells. |
URI: | https://opendata.uni-halle.de//handle/1981185920/88327 http://dx.doi.org/10.25673/86374 |
Open Access: | Open access publication |
License: | (CC BY 4.0) Creative Commons Attribution 4.0 |
Sponsor/Funder: | Publikationsfonds MLU |
Journal Title: | Results in chemistry |
Publisher: | Elsevier |
Publisher Place: | Amsterdam |
Volume: | 4 |
Original Publication: | 10.1016/j.rechem.2022.100371 |
Appears in Collections: | Open Access Publikationen der MLU |
Files in This Item:
File | Description | Size | Format | |
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1-s2.0-S221171562200090X-main.pdf | 821.8 kB | Adobe PDF | View/Open |