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

Shigeki Sasaki, Takeru Ehara, Md Rowshon Alam, Yasuhiro Fujino, Naozumi Harada, Junko Kimura, Hideo Nakamura, Minoru Maeda

Research output: Contribution to journalArticlepeer-review

9 Citations (Scopus)

Abstract

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 0.3 μM. A hypothetical binding model for the new inhibitors has been proposed based on the structure-activity relationship.

Original languageEnglish
Pages (from-to)2581-2584
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume11
Issue number19
DOIs
Publication statusPublished - Oct 8 2001

All Science Journal Classification (ASJC) codes

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

Fingerprint Dive into the research topics of 'Solid-phase synthesis of a library constructed of aromatic phosphate, long alkyl chains and tryptophane components, and identification of potent dipeptide telomerase inhibitors'. Together they form a unique fingerprint.

Cite this