Synthesis and cytotoxic activity of 2-acyl-1H-indole-4,7-diones on human cancer cell lines.

Mahboobi S; Sellmer A; Eichhorn E; Beckers T; Fiebig HH; Kelter G

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Synthesis and cytotoxic activity of 2-acyl-1H-indole-4,7-diones on human cancer cell lines.

机译：2-酰基-1H-吲哚-4,7-二酮的合成及其对人癌细胞系的细胞毒活性。

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Synthesis and cytotoxic activity of a series of 2-acyl-1H-indole-4,7-diones on human cancer cell lines are described. Due to close structural relationship to 2-acylindoles, potent inhibitors of tubulin polymerization, the mode of action of these novel compounds has been investigated. Cytotoxicity, the influence on tubulin polymerization, and cell cycle dependent cytotoxicity on colon carcinoma cells by investigation of RKO exo p27 versus RKO p27(kip1) cells are described. IC50 values of arrested versus proliferating cells differ only in a range of two to fourfold and therefore cellular targets, predominantly relevant for mitotic progression, are excluded. As shown by the significant difference in the IC90 values on different tumor cell lines, the investigated compounds seem to act selectively on mammary and renal cancer cells.

机译：描述了一系列2-酰基-1H-吲哚-4,7-二酮对人类癌细胞系的合成和细胞毒活性。由于与微管蛋白聚合的有效抑制剂2-酰基环吲哚的紧密结构关系，已经研究了这些新型化合物的作用方式。通过研究RKO exo p27与RKO p27（kip1）细胞，描述了结肠癌细胞的细胞毒性，对微管蛋白聚合的影响以及细胞周期依赖性细胞毒性。停滞细胞与增殖细胞的IC50值仅相差2到4倍，因此排除了主要与有丝分裂进程有关的细胞靶标。如不同肿瘤细胞系上IC90值的显着差异所示，所研究的化合物似乎对乳腺和肾癌细胞具有选择性作用。

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来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2005年第1期|共8页
作者
Mahboobi S; Sellmer A; Eichhorn E; Beckers T; Fiebig HH; Kelter G;
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正文语种 eng
中图分类基础医学;
关键词
Tumor cells; malignant; Synthesis; indole-4; 7-dione; Human;

机译：肿瘤细胞;恶性;合成;吲哚-4;7-二酮;人类;

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1. Synthesis and cytotoxic activity of 2-acyl-1H-indole-4,7-diones on human cancer cell lines. [J] . Mahboobi S, Sellmer A, Eichhorn E, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2005,第1期

机译：2-酰基-1H-吲哚-4,7-二酮的合成及其对人癌细胞系的细胞毒活性。
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Synthesis and cytotoxic activity of 2-acyl-1H-indole-4,7-diones on human cancer cell lines.

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