• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Anti-Cancer Drug Design >Dimeric analogues of non-cationic tricyclic aromatic carboxamides are a new class of cytotoxic agents.
【24h】

Dimeric analogues of non-cationic tricyclic aromatic carboxamides are a new class of cytotoxic agents.

机译：非阳离子三环芳族羧酰胺的二聚体类似物是一类新的细胞毒性剂。

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

A series of tricyclic aromatic carboxamides, and their corresponding dimeric analogues, were prepared and their growth-inhibitory properties were evaluated in a series of cell lines. The dimeric compounds were prepared by reaction of the appropriate acids with carbonyl-1,1'-diimidazole, isolating the resulting imidazolides, and reacting these with a stoichiometric amount of the diamine. The monomeric carboxamides containing a (CH2)2NMe2 side chain had widely differing inhibitory potencies, with the known nitronaphthalimide (mitonafide) and acridine-4-carboxamide (DACA) being the most potent. The corresponding bis analogues, linked by a (CH2)3NMe(CH2)3 chain, were generally more potent, with the largest increases (dimer/monomer ratio 20- to 30-fold) seen for the nitronaphthalimides and the phenazines. Based on the intrinsic cytotoxicity of the monomers and the highest degree of increase in cytotoxicity on dimerization, the most interesting chromophores appear to be the acridine-4-carboxamide and phenazine-1-carboxamide. Both of these compounds showed significant growth delays (approximately 6 days) in an in vivo colon 38 tumour model in mice.
机译：制备了一系列三环芳族羧酰胺及其相应的二聚体类似物，并在一系列细胞系中评估了它们的生长抑制特性。通过使合适的酸与羰基-1,1'-二咪唑反应，分离所得的咪唑化物，并使它们与化学计量的二胺反应来制备二聚化合物。含有（CH2）2NMe2侧链的单体羧酰胺具有广泛不同的抑制能力，其中已知的硝基萘二甲酰亚胺（mitonafide）和a啶-4-羧酰胺（DACA）最有效。通过（CH2）3NMe（CH2）3链连接的相应的双类似物通常更有效，对于硝基萘二甲酰亚胺和吩嗪类化合物，其增加最大（二聚体/单体比为20至30倍）。基于单体的固有细胞毒性和二聚作用时细胞毒性增加的最高程度，最有趣的生色团似乎是a啶-4-甲酰胺和吩嗪-1-甲酰胺。这两种化合物在小鼠体内结肠38肿瘤模型中均显示出显着的生长延迟（约6天）。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号