Specific stabilization of DNA triple helices by indolo[2,1-b]quinazolin-6,12-dione derivatives
Resource
Bioorg Med Chem Lett,17,1769-1772.
Journal
Bioorganic & Medicinal Chemistry Letters
Pages
1769-1772
Date Issued
2007-12
Date
2007-12
Author(s)
Chen, GS
Bhagwat, BV
Liao, PY
Chen, HT
Lin, SB
Chern, JW.
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. © 2006 Elsevier Ltd. All rights reserved.
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