Graduate Institute of Life Sciences, National Defense Medical Center, Taipei 114, Taiwan.
Eur J Med Chem. 2012 Apr;50:102-12. doi: 10.1016/j.ejmech.2012.01.044. Epub 2012 Feb 1.
A series of symmetrical disubstituded 1,8-diamidoanthraquinones were synthesized and evaluated for anti-proliferation, telomerase inhibitory by TRAP assay, and hTERT expression by SEAP assay. All of the compounds tested, except for compounds 3a and 3s were selected by the NCI screening system. In addition, compounds 4e and 4k exhibited inhibitory effects on telomerase activity. Taken together, our findings indicated that the analysis of cytotoxicity and telomerase inhibition might provide information applicable for further developing potential telomerase targeting strategy.
一系列对称取代的 1,8-二酰胺基蒽醌被合成，并通过 TRAP assay 评估其抗增殖、端粒酶抑制以及 SEAP assay 评估 hTERT 表达的活性。除化合物 3a 和 3s 外，所有测试的化合物均通过 NCI 筛选系统进行了选择。此外，化合物 4e 和 4k 表现出对端粒酶活性的抑制作用。综上所述，我们的研究结果表明，细胞毒性和端粒酶抑制分析可能提供适用于进一步开发潜在的端粒酶靶向策略的信息。
