Synthesis and antitumor activity of[6/6]sesquiterpene derivatives
OBJECTIVE To synthesize[6/6]sesquiterpenoid derivatives and test their antitumor activity.METHODS The[6/6]sesquiterpene skeleton was constructed by a 7 step reaction using 5-chloro-1-pentyne and 3-methyl-2-cyclohexen-1-one as raw materials,and then using esterification reaction,five[6/6]sesquiterpene derivatives were obtained.The inhibitory effects of the target compounds on human cervical cancer Hela cells,human non-small cell lung cancer A549 cells,and human bladder cancer 5637 cells were determined using CCK-8 assay.RESUITS The target compounds showed different degrees of inhibitory effects on the above three types of tumor cells.Among them,compound Ⅱ showed significant inhibitory effects on Hela cells and 5637 cells,and compound Ⅰ c on A549 cells,with IC50 of 17.28,16.99 and 14.72 µg·mL-1,respectively.CONCLUSION The analysis of the conformational relationship results of the target compounds synthesized can provide a reference basis for the structural optimization of the[6/6]sesquiterpene antitumor drugs.
[6/6]sesquiterpenesDerivativesSynthesizeStructural frameworkAntitumor activityADMET calculateEsterificationHuman bladder cancer cells
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