Selective and low-cost triterpene urea and amide derivatives of high cytotoxicity and selectivity

Abstract

Phytochemicals play a vital role in drug discovery, especially for the development of anti-cancer drugs. Thereby, convenient syntheses, high cytotoxicity but also good tumor cell/non-tumor cell selectivity, are called for. An interesting group of phytochemicals is represented by pentacyclic triterpenoic acids and derivatives thereof. Herein we report the synthesis of some ursolic and oleanolic acid derived amides and urea derivatives and the results from sulforhodamine (SRB) assays to assess their cytotoxic activity for several human tumor cell lines. As a result, an ursolic acid derived benzyl urea 16 showed a rather low EC50 = 1.4 μM for A375 melanoma cell while being not cytotoxic (EC50 = 70 μM) for non-malignant fibroblasts (NIH 3T3).

Keywords

• Triterpenoic Acids
• Cytotoxicity
• Urea