Synthesis and evaluation of 9-aminoacridines derived from benzyne click chemistry

被引:16
|
作者
Howell, Lesley A. [1 ]
Howman, Aaron [1 ]
O'Connell, Maria A. [1 ]
Mueller, Anja [1 ]
Searcey, Mark [1 ]
机构
[1] Univ E Anglia, Sch Pharm, Norwich NR4 7TJ, Norfolk, England
关键词
DNA; Threading intercalators; Acridines; Benzyne click chemistry; TOPOISOMERASE-II; CRYSTAL-STRUCTURE; AGENTS; AZIDES; D(CGTACG)(2); BINDING;
D O I
10.1016/j.bmcl.2009.08.070
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A small set of 9-aminoacridine-3- and 4-carboxamides were synthesized efficiently using the benzyne/azide click chemistry. The products bind to duplex DNA but have different antitumour activity in the HL60 cell line. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码:5880 / 5883
页数:4
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