Solid-Phase synthesis of a library constructed of aromatic phosphate, long alkyl chains and tryptophane components, and identification of potent dipeptide telomerase inhibitors

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• 作者：Sasaki ; Shigeki ; Ehara ; Takeru ; Rowshon Alam ; Md ; Fujino ; Yasuhiro ; Harada ; Naozumi ; Kimura ; Junko ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2001
• 出版时间：October 8, 2001
• 年：2001
• 卷：11
• 期：19
• 页码：2581-2584
• 全文大小：188 K

文摘

Telomerase inhibitors are expected as a new candidate of therapeutic agents for cancer. Recently, we have found novel inhibitors based on the bisindole skeleton. In this study, solid-phase synthesis was applied to construct a library of inhibitors having aromatic phosphate, long alkyl chain and tryptophane components, from which a d,d-ditryptophane derivative has been identified as a new potent telomerase inhibitor with IC₅₀ values of 0.3μM. A hypothetical binding model for the new inhibitors has been proposed based on the structure–activity relationship.