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结构类似物的 Schweinfurthin F:探测 D-环亚结构的空间位阻、电子和疏水性。

Structural analogues of schweinfurthin F: probing the steric, electronic, and hydrophobic properties of the D-ring substructure.

机构信息

Department of Chemistry, University of Iowa, Iowa City, IA 52242-1294, USA.

出版信息

Bioorg Med Chem. 2010 Feb 15;18(4):1676-83. doi: 10.1016/j.bmc.2009.12.063. Epub 2010 Jan 4.

Abstract

The natural tetracyclic schweinfurthins are potent and selective inhibitors of cell growth in the National Cancer Institute's 60-cell line screen. An interest in determination of their cellular or molecular target has inspired our efforts to prepare both the natural products and analogues. In this paper, chemical synthesis of analogues modified in different olefinic positions, and preliminary results from studies of their biological activity, are reported.

摘要

天然四环喜树素是国立癌症研究所 60 细胞系筛选中具有强大和选择性的细胞生长抑制剂。由于对确定其细胞或分子靶标感兴趣,这激发了我们制备天然产物和类似物的努力。本文报道了不同位置的烯烃修饰类似物的化学合成及其生物活性研究的初步结果。

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