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选定异α-咔啉的构效关系研究。I.

Structure-activity relationship studies on selected iso-alpha-carbolines. I.

作者信息

Peczyńska-Czoch W, Mordarski M, Kaczmarek L, Nantka-Namirski P

出版信息

Arch Immunol Ther Exp (Warsz). 1986;34(3):327-31.

PMID:3296992
Abstract

In the course of microbial transformation of the antitumor compounds, it has been found that iso-alpha-carbolines and their certain derivatives undergo N-1 methylation by Kitasatosporia setae. The resulting products, iso-alpha-carbolines exhibit antibacterial and antifungal properties in the concentration range of 0.2-2.5 mumol/ml. In the cytotoxicity test only derivatives substituted at C-2 and C-4 display moderate activity against KB cells. None of the compounds tested show a significant inhibitory effect against P388 lymphocytic leukemia.

摘要

在抗肿瘤化合物的微生物转化过程中,已发现异α-咔啉及其某些衍生物会被刺孢北里孢菌进行N-1甲基化。所得产物异α-咔啉在0.2 - 2.5 μmol/ml的浓度范围内表现出抗菌和抗真菌特性。在细胞毒性试验中,只有在C-2和C-4位被取代的衍生物对KB细胞表现出中等活性。所测试的化合物均未对P388淋巴细胞白血病显示出显著的抑制作用。

相似文献

1
Structure-activity relationship studies on selected iso-alpha-carbolines. I.选定异α-咔啉的构效关系研究。I.
Arch Immunol Ther Exp (Warsz). 1986;34(3):327-31.
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Microbial transformation of azacarbazoles. VII. Antitumor properties of benzo-alpha-iso-carbolines formed by Kitasatosporia setae strain from corresponding benzo-alpha-carbolines.氮杂咔唑的微生物转化。VII. 由浅黄游动放线菌菌株从相应的苯并-α-咔啉形成的苯并-α-异咔啉的抗肿瘤特性。
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Microbial transformation of azacarbazoles. III. Conversion of methoxy- and phenyl- substituted alpha-carbolines to corresponding alpha-iso-carbolines by Kitasatosporia setae strain.氮杂咔唑的微生物转化。III. 北里孢菌菌株将甲氧基和苯基取代的α-咔啉转化为相应的α-异咔啉
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Microbial transformation of azacarbazoles. II. Conversion of methyl-substituted alpha-carbolines to corresponding alpha-iso-carbolines by Kitasatosporia setae strain.氮杂咔唑的微生物转化。II. 北里孢菌菌株将甲基取代的α-咔啉转化为相应的α-异咔啉
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