Synthesis and cytotoxic activity of a new series of topoisomerase I inhibitors

被引：22

作者：

Dallavalle, Sabrina ^{[1
]}

Gattinoni, Sonia ^{[1
]}

Mazzini, Stefania ^{[1
]}

Scaglioni, Leonardo ^{[1
]}

Merlini, Lucio ^{[1
]}

Tinelli, Stella ^{[2
]}

Beretta, Giovanni L. ^{[2
]}

Zunino, Franco ^{[2
]}

机构：

[1] Univ Milan, Dipartimento Sci Mol Agroaliment, I-20133 Milan, Italy

[2] Ist Nazl Tumori, Fondaz IRCCS, Dept Expt Oncol & Labs, I-20133 Milan, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 04期

关键词：

D O I：

10.1016/j.bmcl.2007.12.055

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of structurally simple analogues of natural topopyrone C were synthesized and tested for cytotoxic and topoisomerase I inhibitory activities. The removal of the hydroxyl groups at the 5 and 9 positions resulted in an increased cytotoxic potency and ability to stabilize topoisomerase-mediated cleavage. In addition, the results suggest that some structural features, such as the pyrone ring and a polar group in position 11, are fundamental for topoisomerase I inhibitory effect. These structural requirements are also consistent with the cytotoxic activity. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：1484 / 1489

页数：6

共 15 条

[1] Molecular rearrangement of some o-acyloxyacetophenones and the mechanism of the production of 3-acylchromones [J].