Vinyldiaminotriazine-acridine conjugate as G-quadruplex alkylating agent

Madoka E. Hazemi, Kazumitsu Onizuka, Tomohito Kobayashi, Akira Usami, Norihiro Sato, Fumi Nagatsugi

Research output: Contribution to journalArticlepeer-review

11 Citations (Scopus)


Higher-order structures of nucleic acids have become widely noted for their biological consequences and the discovery of an alkylating small molecule for these structures has been of interest due to its therapeutic potential. We previously developed the vinyldiaminotriazine (VDAT)-acridine conjugate as a T-T mismatch alkylating agent. In this report, we focused on the finding of the alkylation to the G-quadruplex (G4) DNA with VDAT-acridine conjugates. The VDAT-acridine conjugates exhibited a considerable alkylation ability to G4 under mild conditions. Moreover, the investigation of properties with the alkylated G4 revealed that alkylation by this conjugate significantly increased the stability of the G4 structure. This study provides a starting point in the further development of selective G4 alkylating small molecules.

Original languageEnglish
Pages (from-to)3551-3558
Number of pages8
JournalBioorganic and Medicinal Chemistry
Issue number12
Publication statusPublished - 2018 Jul 23


  • Acridine
  • Alkylating small molecule
  • G-quadruplex
  • Higher-order structures
  • T-T mismatch
  • Telomerase


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