Synthesis and Cytotoxicity of Lupane Mono- and Bis-Piperazinylamides

Mono- and bis-piperazinylamides of lupane acids and their derivatives modified on ring A were synthesized and tested for cytotoxicity. Cytotoxicity studies against nine different human tumor cells found that betulonic acid N -methylpiperazinylamide inhibited the growth of SR leukemia, NCI-H460 non-small-cell lung cancer, and HCT-116 colon cancer cells. Cyanoethyl, hydrazone, and oxime moieties in the C3 position had positive effects on the cytotoxicity. The activity spectrum of acanthochlamic diacid amides was broader. The absence/ presence of an N -ethyl group on the piperazine ring affected the cancer type and breadth of cell lines.