合成 4β-氨甲酰基表鬼臼毒素类化合物作为潜在的抗肿瘤剂。
Synthesis of 4β-carbamoyl epipodophyllotoxins as potential antitumour agents.
机构信息
Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500 607, India.
出版信息
Bioorg Med Chem. 2011 May 1;19(9):2975-9. doi: 10.1016/j.bmc.2011.03.030. Epub 2011 Mar 21.
A series of new 4β-carbamoyl epipodophyllotoxin analogues have been synthesized and evaluated for their anticancer activity against eleven cancer cell lines including Zr-75-1, MCF7, KB, Gurav, DWD, Colo 205, A-549, Hop62, PC3, SiHa and A-2780. Most of the compounds exhibited better growth-inhibition activities against tested cell lines than that of etoposide. Further, compounds 6g and 6i are also evaluated for their DNA topoisomerase-II (topo-II) inhibition activity and they exhibited significant inhibition of topo-II catalytic activity comparable to etoposide.
一系列新的 4β-氨甲酰表鬼臼毒素类似物已经被合成，并对其针对包括 Zr-75-1、MCF7、KB、Gurav、DWD、Colo 205、A-549、Hop62、PC3、SiHa 和 A-2780 在内的十一种癌细胞系的抗癌活性进行了评估。大多数化合物对测试细胞系的生长抑制活性都优于依托泊苷。此外，化合物 6g 和 6i 也被评估了它们对 DNA 拓扑异构酶-II（topo-II）的抑制活性，它们表现出与依托泊苷相当的显著的 topo-II 催化活性抑制作用。
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