Synthesis and cytotoxicity of new alkyne derivatives of pentacyclic triterpenoids

Pentacyclic triterpene hydroxy acids were transformed into acetylene-containing derivatives: propargyl esters at the carboxy group and O-(hex-5-ynoyl) derivatives at the hydroxy group. The cytotoxicity of the synthesized compounds was examined against HepG2 and Huh7 hepatocarcinoma cells and PC3 prostate cancer cells. The primary analysis of the structureactivity relationships was performed; glycyrrhetic acid derivatives showed the maximum enhancement in the cytotoxic properties upon introduction of an alkyne moiety.