杂环连接的 4β-酰胺基鬼臼毒素的合成及其作为凋亡诱导剂的抗癌活性。
Synthesis and anticancer activity of heteroaromatic linked 4β-amido podophyllotoxins as apoptotic inducing agents.
机构信息
Division of Organic Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India.
出版信息
Bioorg Med Chem Lett. 2013 Jan 1;23(1):273-80. doi: 10.1016/j.bmcl.2012.10.099. Epub 2012 Nov 1.
A series of different heteroaromatic linked 4β-amidopodophyllotoxin conjugates (16a-i, 17a-i and 18a-d) were synthesized and evaluated for anticancer activity against five human cancer cell lines. Among the series, one of the compound 17g showed significant antiproliferative activity in A549 (lung cancer) cell line. Flow cytometric analysis showed that 17g arrested the cell cycle in the G2/M phase leading to caspase-3 dependent apoptotic cell death. Further, Hoechst 33258 staining and DNA fragmentation assay also suggests that 17g induces cell death by apoptosis.
一系列不同的杂芳基连接的 4β-酰胺鬼臼毒素缀合物（16a-i、17a-i 和 18a-d）被合成并评估了对五种人癌细胞系的抗癌活性。在该系列中，化合物 17g 对 A549（肺癌）细胞系表现出显著的增殖抑制活性。流式细胞术分析表明，17g 将细胞周期阻滞在 G2/M 期，导致 caspase-3 依赖性凋亡细胞死亡。此外，Hoechst 33258 染色和 DNA 片段化实验也表明，17g 通过凋亡诱导细胞死亡。
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