Synthesis and antitumour activity of glycyrrhetinic acid derivatives

Pentacyclic triterpene derivatives possessing polyhydroxyl ring A inhibit Gram-positive bacteria growth by regulating metabolism and virulence genes expression

“…The hydroxyl triterpene acids (12 or 14) were reacted with different alkyl halides in the solution of K 2 CO 3 /DMF to give two series of ester derivatives with high yields (>95.0 %), respectively, including alkyl esters (linear-chain alkyl ester or branched-chain alkyl ester derivatives) and benzyl esters (nitro-substituted or chloro-substituted benzyl ester derivatives) [14].…”

“…Accordingly, UA was first treated with benzyl bromide in the presence of K 2 CO 3 in DMF to form M A N U S C R I P T A C C E P T E D ACCEPTED MANUSCRIPT 5 benzyl ester (1) [14]. OA and 1 were then oxidized with Jones reagent to produce 3-ketone compounds (2,3) in good yields (>95.0%), followed by another oxidation reaction with selenium dioxide in acetic anhydride to produce α,β-unsaturated ketones (4,5) in moderate yields (about 50.0%) [15,16].…”

Synthesis and Cytotoxic Activity of Methyl Glycyrrhetinate Esterified with Amino Acids

“…Various amino acids of different lengths and structures were attached to carbon C3 while carbon C30 was esterified -based on the results of previous studies [27]. The influence of the substituents on cytotoxicity resulting from the different polarity pattern and lipophilicity along the molecule was studied in sulforhodamine B (SRB) assays.…”

New antitumor 6-chloropurine nucleosides inducing apoptosis and G2/M cell cycle arrest

“…Therefore, also the minor β-mannosyl nucleosides were isolated and tested in order to receive comparable biological data to correlate structure with bioactivity in this family of compounds. The hydroxy groups of the glycosyl moities remained benzylated, since the presence of benzyl groups enhances the cytotoxicity of glycosylated compounds [20,21]. Moreover, benzyl groups represent a suitable metabolic protection.…”