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合成系列 b-咔啉-3-甲酰胺类化合物,并研究其与CT-DNA的作用。以l-色氨酸为原料,设计并合成 b-咔啉-3-甲酰胺类化合物,利用粘度滴定、Tm(解链温度)测定及紫外光谱滴定法以及微量量热等方法测定其与CT-DNA的作用。在与CT-DNA的相互作用中,它们均能引起CT-DNA Tm的改变;粘度滴定实验表明该系列化合物与DNA以嵌插方式作用;紫外光谱滴定法表明该系列化合物与DNA的结合强度是有差异的,这与抗肿瘤筛选的结果一致;微量量热研究结果表明这类化合物与DNA的作用是熵驱动的。该b-咔啉新衍生物是以DNA为靶,并通过与DNA碱基的嵌插产生生物效应。
The series of b-carboline-3-carboxamides were synthesized and their effects on CT-DNA were investigated. To l-tryptophan as raw material, design and synthesis of b-carboline-3-carboxamide compounds, the use of viscosity titration, Tm (melting temperature) and UV spectrophotometry and microcalorimetry and other methods measured with CT The role of DNA. In the interaction with CT-DNA, they can cause CT-DNA Tm changes; viscosity titration experiments show that the series of compounds and DNA intercalation effect; UV spectrophotometry titration showed that the series of compounds and DNA binding strength There is a difference, which is consistent with the results of anti-tumor screening; microcalorimetry results show that the effect of these compounds on DNA is entropy-driven. The new derivatives of b-carboline target DNA and produce biological effects by intercalation with DNA bases.