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多芳基取代 4β-N-派洛立林鬼臼毒素的合成:DNA 拓扑异构酶抑制、抗癌和诱导细胞凋亡活性。

Synthesis of 4β-N-polyaromatic substituted podophyllotoxins: DNA topoisomerase inhibition, anticancer and apoptosis-inducing activities.

机构信息

Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500 607, India.

出版信息

Bioorg Med Chem. 2010 Dec 15;18(24):8493-500. doi: 10.1016/j.bmc.2010.10.042. Epub 2010 Nov 10.

Abstract

A new class of 4β-N-polyaromatic substituted podophyllotoxin congeners have been synthesized and evaluated for their DNA topoisomerase-II (topo-II) inhibition as well as anticancer potential in some human cancer cell lines. The ease of synthesis and interesting biological activities make the present series of polyaromatic-podophyllotoxin congeners as a promising new structure for the development of new anticancer agents based on podophyllotoxin scaffold.

摘要

一类新型的 4β-N-多芳基取代的鬼臼毒素同系物已经被合成,并对其作为 DNA 拓扑异构酶-II(topo-II)抑制剂以及在一些人类癌细胞系中的抗癌潜力进行了评估。由于其合成的简便性和有趣的生物活性,本系列的多芳基-鬼臼毒素同系物有望成为基于鬼臼毒素骨架开发新型抗癌药物的新结构。

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