Tetraplex DNA specific ligands based on the fluorenone-carboxamide scaffold

被引：23
作者：
Alcaro, Stefano
Artese, Anna
Iley, James N.
Maccari, Rosanna
Missailidis, Sotiris
Ortuso, Francesco
Ottana, Rosario
Ragazzon, Patricia
Vigorita, Maria Gabriella
机构：
[1] Magna Graecia Univ Catanzaro, Dipartimento Sci Farmacobiol, I-88021 Roccelletta di Borgia, CZ, Italy
[2] Open Univ, Dept Chem, Milton Keynes MK7 6AA, Bucks, England
[3] Univ Messina, Fac Farm, Dipartimento Farmacochim, I-98168 Messina, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 09期
关键词：
fluorenone-carboxamides; DNA binding; thermal denaturation; UV spectroscopy; competition dialysis; fluorescence spectroscopy; molecular modeling;
D O I：
10.1016/j.bmcl.2007.02.022
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of fluorenone-carboxamide compounds was analyzed with regard to DNA binding properties by UV spectroscopy and competition dialysis methods. The morpholino derivative 10 provided interesting results in terms of affinity and specificity toward the DNA G-tetraplex structures. Interactions against this target were evaluated by a comparative molecular modeling study in agreement with the experimental data, proposing a model for the rational design of new agents with potent and selective DNA tetraplex binding properties. (C) 2007 Elsevier Ltd. All rights reserved.
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收藏
页码：2509 / 2514
页数：6
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