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

被引:13
作者
Chen, Grace Shiahuy
Bhagwat, Bhalchandra V.
Liao, Pei-Yin
Chen, Hui-Ting
Lin, Shwu-Bin
Chern, Ji-Wang [1 ]
机构
[1] Natl Taiwan Univ, Sch Pharm, Coll Med, Taipei 10051, Taiwan
[2] Providence Univ, Dept Appl Chem, Shalu 43301, Taiwan
[3] Natl Taiwan Univ, Dept Clin Lab Sci & Med Biotechnol, Taipei 10051, Taiwan
关键词
DNA triplex; triplex stabilizing agents; tryptanthrin; indolo[2,1-b]quinazolin-6,12-dione; thermal denaturation;
D O I
10.1016/j.bmcl.2006.12.079
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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 degrees 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. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1769 / 1772
页数:4
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