《表1 化合物的体外抗艰难梭菌活性》

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《抗艰难梭菌rakicidin B1新衍生物的设计、合成及生物学活性评价（英文）》

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The data in Tab.3 indicated that analogues 3b had poor anti-tumor activity to Caco-2 cells with IC50 value at 212.0μmol/L，which was 28.3-fold less active than that of rakicidin B1 under normoxic condition.Furthermore，the activity of rakicidin B1 against Caco-2 cells was5-fold more potent than corresponding IC50 value of 3b under hypoxia condition，which furtherly demonstrated the fact that the cytotoxicity of 3b was decreased with the range from single digital（5.0 fold）to ten-digital fold（28.3 fold）under normoxic or hypoxic conditions，respectively.In addition，novel rakicidin B1 analogues showed the hypoxia-selective cytotoxicity against Caco-2 cell lines examined.It was approximately 10-fold more cytotoxic under hypoxic than under normoxic conditions.Compared to normoxic conditions（IC50=212.0μmol/L），rakicidin 3b showed dramatically enhanced cytotoxicity（IC50=3.8μmol/L）under the hypoxic conditions with selectivity value 55.8.Therefore，as our expected，the point of view that hypoxia-selective cytotoxicity of rakicidin analogues was further proved in this part[16].