Parallel synthesis and cytotoxicity evaluation of a polyamine-quinone conjugates library

被引：34

作者：

Bolognesi, Maria Laura ^{[1
]}

Calonghi, Natalia ^{[2
]}

Mangano, Chiara ^{[2
]}

Masotti, Lanfranco ^{[2
]}

Melchiorre, Carlo ^{[1
]}

机构：

[1] Univ Bologna, Dept Pharmaceut Sci, Alma Mater Studiorum, I-40126 Bologna, Italy

[2] Univ Bologna, Dept Biochem G Moruzzi, Alma Mater Studiorum, I-40126 Bologna, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 17期

关键词：

D O I：

10.1021/jm800637b

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A library of 24 derivatives designed by combining two natural products-derived fragments was prepared and tested to determine their anticancer potential in HT29 colon cancer cells. All library members inhibit cell proliferation as measured by MTT mitochondrial functional assay, with IC50 values in the 1-100 mu M range. Entry 1b caused apoptotic EGFR-mediated intracellular signaling. Thus, polyamino-quinones emerged as readily accessible and easily diversified scaffolds for anticancer lead discovery.

引用

页码：5463 / 5467

页数：5

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