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简单盖杷素类似物的合成、细胞毒性及构效关系

Synthesis, cytotoxicity and SAR of simple geiparvarin analogues.

作者信息

Valenti P, Rampa A, Recanatini M, Bisi A, Belluti F, Da Re P, Carrara M, Cima L

机构信息

Department of Pharmaceutical Sciences, University of Bologna, Italy.

出版信息

Anticancer Drug Des. 1997 Sep;12(6):443-51.

PMID:9311554
Abstract

Some simple geiparvarin analogues, in which the coumarin moiety has been replaced with an X-substituted benzene ring, are described. The compounds were tested on LoVo cells (human colon carcinoma cell line) and some of them show a cytotoxicity comparable with that of the prototype. A QSAR analysis was also attempted, but it did not provide satisfactory results, mainly because of the limited range of variation of the biological activity.

摘要

描述了一些简单的盖帕瓦林类似物,其中香豆素部分已被X-取代的苯环所取代。这些化合物在LoVo细胞(人结肠癌细胞系)上进行了测试,其中一些显示出与原型相当的细胞毒性。还尝试了定量构效关系(QSAR)分析,但未得到满意结果,主要是因为生物活性的变化范围有限。

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