Development of novel telomerase inhibitors based on a bisindole unit

Shigeki Sasaki; Takeru Ehara; Ikuhiro Sakata; Yasuhiro Fujino; Naozumi Harada; Junko Kimura; Hideo Nakamura; Minoru Maeda

doi:10.1016/S0960-894X(01)00002-6

Development of novel telomerase inhibitors based on a bisindole unit

Shigeki Sasaki, Takeru Ehara, Ikuhiro Sakata, Yasuhiro Fujino, Naozumi Harada, Junko Kimura, Hideo Nakamura, Minoru Maeda

Chemo-Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

21 Citations (Scopus)

Abstract

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 IC₅₀ values 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.

Original language	English
Pages (from-to)	583-585
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	11
Issue number	4
DOIs	https://doi.org/10.1016/S0960-894X(01)00002-6
Publication status	Published - Feb 26 2001

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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AU - Sasaki, Shigeki

AU - Ehara, Takeru

AU - Sakata, Ikuhiro

AU - Fujino, Yasuhiro

AU - Harada, Naozumi

AU - Kimura, Junko

AU - Nakamura, Hideo

AU - Maeda, Minoru

PY - 2001/2/26

Y1 - 2001/2/26

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AB - 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 IC50 values 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.

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