– CU-CPT17e shows strong NF-?B activation in TLR3, TLR8 and TLR9 HEK293 cells with EC50 values of 4.80±0.73, 13.5±0.58 and 5.66±0.17 ?M, respectively. CU-CPT17e significantly improves the activity with 13.9±0.9 fold of NF-?B activation and an EC50 value of 4.8±0.7 ?M. CU-CPT17e inhibits the proliferation of HeLa cancer cells by triggering apoptosis and arresting the cell cycle at the S phase. The induction of apoptosis by CU-CPT17e in HeLa cells is investigated. HeLa cells are cultured with increasing concentrations of CU-CPT17e or poly I:C or blank control (DMSO) for 24 h. Treatment with CU-CPT17e for 24 h at different concentrations (10 to 40 ?M) results in an elevation of apoptotic cell population ranging from 10% to 17%, which is more effective than poly I:C at 5 ?g/mL. These results suggest that the antiproliferative activity of CU-CPT17e against HeLa cells might result from its ability to directly induce apoptosis[1].