Synthesis and Telomeric G-Quadruplex-Stabilizing Ability of Macrocyclic Hexaoxazoles Bearing Three Side Chains

• 広川, 貴次

• Ma, Yue

• Iida, Keisuke

• Sasaki, Shogo

• Heddi, Brahim

• Phan, Anh

• Nagasawa, Kazuo

抄録

G-quadruplexes (G4s), which are structures formed in guanine-rich regions of DNA, are involved in a variety of significant biological functions, and therefore “sequence-dependent” selective G4-stabilizing agents are required as tools to investigate and modulate these functions. Here, we describe the synthesis of a new series of macrocyclic hexaoxazole-type G4 ligand (6OTD) bearing three side chains. One of these ligands, 5b, stabilizes telomeric G4 preferentially over the G4-forming DNA sequences of c-kit and K-ras, due to the interaction of its piperazinylalkyl side chain with the groove of telomeric G4.

収録刊行物

• Molecules

  Molecules 24 (2), 263-, 2019-01

  MDPI

キーワード

• Chemistry (miscellaneous)
• Analytical Chemistry
• Organic Chemistry
• Physical and Theoretical Chemistry
• Molecular Medicine
• Drug Discovery
• Pharmaceutical Science

詳細情報

• CRID: 1050283688374113024
• NII論文ID: 120007133102
• DOI: 10.3390/molecules24020263
• ISSN: 14203049
• HANDLE: 2241/00159256
• Web Site: https://tsukuba.repo.nii.ac.jp/records/53838
• Web Site: http://www.mdpi.com/1420-3049/24/2/263/pdf
• 本文言語コード: en
• 資料種別: journal article
• データソース種別:
  • IRDB
  • Crossref
  • CiNii Articles
  • KAKEN