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首页> 外文期刊>Environmental toxicology and chemistry >STRUCTURE-ACTIVITY RELATIONSHIP FOR BROMOINDOLE CARBALDEHYDES: EFFECTS ON THE SEA URCHIN EMBRYO CELL CYCLE
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STRUCTURE-ACTIVITY RELATIONSHIP FOR BROMOINDOLE CARBALDEHYDES: EFFECTS ON THE SEA URCHIN EMBRYO CELL CYCLE

机译:溴吲哚羧酸盐的结构-活性关系:对海豚胎胚细胞周期的影响

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Natural derivatives of indole-3-carbaldehyde were isolated from the tropical marine ascidian Stomoza murrayi. A series of 13 derivatives, three natural and 10 synthetic(brominated and N-methylated), were examined for their effects on cell division of sea urchin eggs. These derivatives were shown to inhibit the first mitotic cycle in a concentration-dependent manner. By comparing the IC50 values with the structure of the various molecules, we were able to determine that bromination increase the cytotoxicity of the compound with a maximum occurring when bromine was added to carbon number 2, while addition of N-methylation was shown to markedly reduce the cytotoxicity of these same compounds brominated at carbon 2 only.
机译:吲哚-3-甲醛的天然衍生物是从热带海洋海生植物Stomoza murrayi中分离出来的。研究了一系列13种衍生物,3种天然衍生物和10种合成衍生物(溴化和N-甲基化)对海胆卵细胞分裂的影响。这些衍生物显示出以浓度依赖性方式抑制第一个有丝分裂周期。通过将IC50值与各种分子的结构进行比较,我们能够确定溴化增加了化合物的细胞毒性,当将溴添加到2号碳原子时,溴化作用最大,而N-甲基化的添加明显降低了溴化作用。这些相同化合物的细胞毒性仅在碳2处溴化。

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