Development of novel telomerase inhibitors based on a bisindole unit.
Development of novel telomerase inhibitors based on a bisindole unit.
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开发基于双吲哚单元的新型端粒酶抑制剂。
DOI：
10.1016/s0960-894x(01)00002-6
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发表时间：
2001
影响因子：
2.7
通讯作者：
M. Maeda
中科院分区：
文献类型：
--
作者：
S. Sasaki;T. Ehara;I. Sakata;Y. Fujino;N. Harada;J. Kimura;H. Nakamura;M. Maeda
端粒酶是延长染色体末端端粒重复序列的酶。由于在大多数癌细胞中观察到高端粒酶活性，人端粒酶抑制剂已被期望作为新的癌症化疗药物。在这里，我们描述了新的抑制剂的IC 50值在亚微摩尔范围内的发现。新的抑制剂的结构将是有用的作为一个支架的库的建设在寻找端粒酶抑制剂。
Telomerase is the enzyme that elongates telomere repeat at the ends of a chromosome. As high telomerase activity is observed in most cancer cells, inhibitors of human telomerase have been expected as new chemotherapeutic agents for cancer. We describe here the discovery of novel inhibitors with IC50values in the submicromolar range. The structure of the novel inhibitors will be useful as a scaffold for construction of the library in the search for telomerase inhibitors.