Synthesis and cytotoxicity of apoptosis-inducing N-heterocyclic triterpene amides

Abstract

The modification of lipophilic triterpenes to enhance their cytotoxicity, is a viable strategy for finding new anti-cancer agents. Herein we report the synthesis, analysis of 18 pentacyclic triterpenoic acid N-heterocyclic amides and their cytotoxicity, tumor cell/non-tumor cell selectivity, as well as their putative mode of action. EC50 values were measured by SRB-assays, and found to be as low as 3.13 ​μM, with a selectivity as high as S ​= ​5.05. Moreover, supportive assays were performed to further analyze their cytotoxicity; these experiments showed the compounds to act mainly by apoptosis.

Keywords

• Triterpenoic acids
• Cytotoxicity
• Amides