| The malignant tumor is one kind of serious disease to threaten the human health at present, cancer preventing and remedying work has become a hot and difficult topic which the various countries’ scientist studied. Chemistry medicine is very important to treatment of cancer. The medicine chemist are interest in good anti-tumor activeness of the sea alkaloid.As a result of its structure complexity, it is intermingled good and evil of the active effect, and it is not often also easy to gain and the side effect is big. Therefore, we have finished structural modification to its kind of compound through the chemical synthesis method to obtain the more ideal medicine activeness and the preparation method.The paper has carried on the design, the synthesis and the anti-tumor activeness test of β-carboline. It is finished22β-carboline kind of goal compound respectively take the indol,6-bromine indol,5-methoxy tryptamine as the starting material,19compounds are pharmacologically active tested. It is16new compounds in which. The goal product have confirmed by the infrared spectrum, the nuclear magnetic resonance hydrogen spectrum, the nuclear magnetic resonance carbon spectrum and the mass spectrum.After the initial anti-tumor activity tests in vivo, the experiment results show that GDT01-GDT03, GDT08, GDT12-GDT19have obvious anti-tumor activity, but GDT04-GDT07, GDT09-GDT11is not. And which completely fragrant β-carboline compound activeness must generally be higher than the four hydrogen β-carboline compounds. The tumor suppression rate of the completely fragrant β-carboline compound are above30%, among of them which GDT16, GDT17, GDT18reach above40%; Anti-tumor suppression rate of the compounds which the position of the sixth are substituted by the methoxy group is generally higher than the compound which not. Anti-tumor suppression rate of β-carboline compound which the aromatic ring has attracts the electricity subbasis such as nitryl is generally lower than the compound which not. |
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