The synthesis of some head to head linked DNA minor groove binders
The synthesis of some head to head linked DNA minor groove binders
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DOI：
10.1016/s0040-4020(00)00432-4
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发表时间：
2000-07-14
期刊：
影响因子：
2.1
通讯作者：
Wylie, WA
中科院分区：
文献类型：
--
作者：
Khalaf, AI;Pitt, AR;Wylie, WA
制备了一系列头对头连接的杂环氨基酸二聚体，用于研究其与DNA小沟结合的亲和力和选择性。用于合成的靶标的选择由基于计算机的设计引导。已经包括了几种新的二羧酸连接体，包括吲哚、菲、芴酮和二苯并噻吩。通过足迹法分析与DNA的结合显示出对衍生自2，7-二氢菲二羧酸的化合物的高亲和力和对含有至少4个AT对但具有跨越多达两个CG碱基对的能力的AT富集区域的主要选择性。(C)2000爱思唯尔科技有限公司版权所有。
A series of head to head linked dimers of heterocyclic amino acids has been prepared for investigation of affinity and selectivity in binding to the minor groove of DNA. The selection of targets for synthesis was led by computer based design. Several novel dicarboxylic acid linkers including indoles, phenanthrenes, a fluorenone, and a bisbenzothiophene have been included. Analysis of binding to DNA by footprinting showed high affinity for compounds derived from 2,7-dihydrophenanthrene dicarboxylic acid and a predominant selectivity for AT rich regions containing at least 4 AT pairs but with the ability to span up to two CG base pairs. (C) 2000 Elsevier Science Ltd. All rights reserved.