Design,synthesis and activities of harringtonine derivatives
In order to discover compounds with good anti-leukemic activity,a total of fifteen harringtonine derivatives were designed and synthesized and their anti-proliferative activity on HL-60 cells were evaluated.The target compounds LY-1-LY-15 were synthesized by nucleophilic substitution,reduction and Mitsunobu reaction using cephalotaxine as the starting material.The structures of the target compounds were confirmed by ESI-MS and 1H-NMR spectra.The anti-proliferative activities of the target compounds against HL-60 cells were tested by Trypan blue staining method.Compound LY-1 showed the strongest inhibitory activity against HL-60 cells with IC50 value of 3.54 μmo1·L-1,which was worthy of further study.
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