Design and semisynthesis of novel fredericamycin A derivatives with an improved antitumor profile

被引:20
作者
Abel, Ulrich
Simon, Werner
Peter, Eckard
Hansske, Friedrich G.
机构
[1] Discovery Partners Int GmbH, D-69123 Heidelberg, Germany
[2] Santhera Pharmaceut, D-69120 Heidelberg, Germany
关键词
fredericamycin; antitumor; spiro quinone; natural product; semisynthesis;
D O I
10.1016/j.bmcl.2006.03.029
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
We report the design, semisynthesis, and biological activity of a series of fredericamycin (1) derivatives. Within this series compound 1e combines low nanomolar cytotoxic potency in vitro, increased tumor cell line selectivity, and in vivo activity in a human xenograft model. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3292 / 3297
页数:6
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