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双吲哚衍生物的抗肿瘤活性及 COMPARE 分析。

Antitumor activity and COMPARE analysis of bis-indole derivatives.

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Bologna, Via Belmeloro 6, 40126 Bologna, Italy.

出版信息

Bioorg Med Chem. 2010 May 1;18(9):3004-11. doi: 10.1016/j.bmc.2010.03.063. Epub 2010 Mar 28.

Abstract

This paper reports the synthesis of new derivatives (formed by two indole systems separated by a central moiety) analogous of potent antitumor agents previously described. The activity of the bis-indoles bearing a pyridine core confirms the good result described in the previous paper and compound 4c was chosen for the first in vivo experiment (Hollow Fiber Assay). COMPARE analysis and structure-activity relationships were also considered. Contrary to data reported by other Authors, no correlations were found between antitumor activity and NQO1 induction.

摘要

本文报道了新型衍生物(由两个吲哚系统通过中心部分隔开形成)的合成,这些衍生物类似于先前描述的有效抗肿瘤剂。带有吡啶核心的双吲哚的活性证实了前一篇论文中描述的良好结果,并且选择化合物 4c 进行第一次体内实验(空心纤维测定)。还考虑了比较分析和构效关系。与其他作者报道的数据相反,未发现抗肿瘤活性与 NQO1 诱导之间存在相关性。

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