Synthesis and antitumor activity evaluation of hederacolchiside A1 derivatives
In order to discover new candidates with good antitumor activity,twenty-two compounds(4a-4k and 5a-5k)were designed and synthesized with hederacolchiside A1 as the lead compound using semi-synthetic strategy to introduce piperazine moieties at C-28.The structures of target compounds were confirmed by ESI-MS,1H-NMR and 13C-NMR.With hederacolchiside A1 and 5-fluorouracil as the positive control drugs,all target compounds were evaluated for in vitro antitumor activities against human tumor cell lines as HCT116,A549,HL-60 and MCF-7 using the MTT colorimetric assay.The results showed that most of the hederacolchiside A1 derivatives containing formylated piperazine structures showed varying degrees of anti-proliferative activities against the tested tumor cell lines.Compound 5e exhibited excellent anti-proliferation activity against MCF-7 cells with IC50 value of(4.89±0.09)µmol·L-1 compared with the positive control drugs,and it could be developed for further research.
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