Oleanolic and ursolic acids are two ubiquitous isomeric triterpene phytochemicals known for their anticanceractivity. A set of derivatives of the two compounds with a modified oxidation state and lipophylicity at C-3 andC-28 positions, were prepared and tested as anticancer agents versus the lines HepG2, Hep3B and HA22T/VGHof hepatocarcinoma, a strongly aggressive tumor that is not responsive toward the standard therapies. Newderivatives containing a three carbons side chain on the C-3 position were synthetized in both stereoisomericforms by the Barbier-Grignard procedure and three of them were found to be active toward all of the threetargets. The implication of the transcriptional nuclear factor NF−κB in the mechanism of action was assessed forthe more active compounds in the set, as hepatocellular carcinoma (HCC) cyto-types are known to overexpressNF−κB.
|Numero di pagine||8|
|Stato di pubblicazione||Published - 2019|
All Science Journal Classification (ASJC) codes
- Molecular Biology
- Drug Discovery
- Organic Chemistry