Specific stabilization of DNA triple helices by indolo[2,1-b]quinazolin-6,12-dione derivatives

Grace Shiahuy Chen, Bhalchandra V. Bhagwat, Pei Yin Liao, Hui Ting Chen, Shwu Bin Lin, Ji Wang Chern*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

13 Scopus citations

Abstract

Derivatives of indolo[2,1-b]quinazolinone containing aminoalkylamino side chains were synthesized as specific DNA triplex stabilizing agents. The aminoalkylamino side chains are essential for triplex stabilization. The position-8 fluorine atom or a methyl group to the nitrogen adjacent to the planar core can enhance triplex stability by 6 °C and the effect is additive. Conformational analysis reveals that the orientation of the side chain underlies the ability of this compound to stabilize a DNA triplex.

Original languageEnglish
Pages (from-to)1769-1772
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number6
DOIs
StatePublished - 15 Mar 2007

Keywords

  • DNA triplex
  • Indolo[2,1-b]quinazolin-6,12-dione
  • Thermal denaturation
  • Triplex stabilizing agents
  • Tryptanthrin

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