Synthesis and biological evaluation of novel 1-O- and 14-O-derivatives of oridonin as potential anticancer drug candidates

Novel 1-O- and 14-O-derivatives of oridonin were synthesized and biologically evaluated. All of the derivatives exhibited stronger cytotoxicity against six cancer cell lines (BGC-7901, SW-480, HL-60, BEL-7402, A549, and B16) than oridonin in vitro, and some of them were more potent than oridonin and cyclophosphamide in vivo. Compounds Ib and IIg were the most potent with the IC50 values of 0.84 μM for Ib in HL-60 cell and 1.00 μM for IIg in BEL-7402 cell.

1-O- and 14-O-derivatives of oridonin exhibited stronger cytotoxicity against six cancer cell lines than oridonin in vitro, compounds Ib and IIg were more potent than oridonin and cyclophosphamide in vivo.Figure optionsDownload as PowerPoint slide