Anti-tumor-promoter activity of modified glycyrrhetinic acid derivatives. Synthesis and structure-activity relationships

Article abstract of DOI:10.1016/0223-5234(92)90088-I

A series of modified derivatives of 18α- and 18β-glycyrrhetinic acid was systematically synthesized and their structure-activity relationships investigated for inhibition of the promoter activity of 12-O-tetradecanoylphorbol-13-acetate in vitro. Increased hydrophobicity in the A-ring moiety and the presence of an 11-oxo function were shown to be important for the high inhibition. Replacement of the carboxy to the hydroxymethyl group at the 20-position also enhanced the inhibitory activity.