4β-烷基酰胺查尔酮和 4β-肉桂酰胺连接的鬼臼毒素的合成及作为凋亡诱导剂的抗癌活性。
Synthesis and anticancer activity of 4β-alkylamidochalcone and 4β-cinnamido linked podophyllotoxins as apoptotic inducing agents.
机构信息
Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500 607, India.
出版信息
Eur J Med Chem. 2012 Jan;47(1):530-45. doi: 10.1016/j.ejmech.2011.11.024. Epub 2011 Nov 20.
A series of 4β-alkylamidochalcone and 4β-cinnamido linked podophyllotoxin congeners have been synthesized. All the twenty nine compounds were evaluated for anticancer activity against five human cancer cell lines (A-549, A375, MCF-7, HT-29 and ACHN). Some of the synthesized compounds showed good anticancer activity that is comparable to etoposide. The IC(50) of compounds 17a and 17f is 2.7 and 2.1 μM respectively against A-549 cancer cell line. Flow cytometric analysis showed that these two compounds 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 suggested that 17a and 17f induced cell death by apoptosis.
已经合成了一系列 4β-烷基酰胺查尔酮和 4β-肉桂酰基连接的鬼臼毒素同系物。对这 29 种化合物进行了抗五种人类癌细胞系（A-549、A375、MCF-7、HT-29 和 ACHN）的抗癌活性评估。一些合成的化合物表现出与依托泊苷相当的良好抗癌活性。化合物 17a 和 17f 对 A-549 癌细胞系的 IC50 分别为 2.7 和 2.1μM。流式细胞术分析表明，这两种化合物将细胞周期阻滞在 G2/M 期，导致 caspase-3 依赖性细胞凋亡。此外，Hoechst 33258 染色和 DNA 片段化分析也表明，17a 和 17f 通过细胞凋亡诱导细胞死亡。
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