• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and Identification of a new class of antileukemic agents containing 2-(arylcarboxamide)-(S)-6-amino-4,5,6,7-tetrahydrobenzo(d)thiazole.
【24h】

Synthesis and Identification of a new class of antileukemic agents containing 2-(arylcarboxamide)-(S)-6-amino-4,5,6,7-tetrahydrobenzo(d)thiazole.

机译：合成和鉴定了一种新型的2-（芳基羧酰胺）-（S）-6-氨基-4,5,6,7-四氢苯并（d）噻唑类抗白血病药物。

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

Recently we have reported the effect of (S)-6-aryl urea/thiourea substituted-2-amino-4,5,6,7-tetrahydrobenzo[d]thiazole derivatives as potent anti-leukemic agents. To elucidate further the Structure Activity Relationship (SAR) studies on the anti-leukemic activity of (S)-2,6-diamino-4,5,6,7-tetrahydrobenzo[d]thiazole moiety, a series of 2-arlycarboxamide substituted-(S)-6-amino-4,5,6,7-tetrahydrobenzo[d]thiazole were designed, synthesized and evaluated for their anti-leukemic activity by trypan blue exclusion, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), lactate dehydrogenase (LDH) assays and cell cycle analysis. Results suggest that the position, number and bulkiness of the substituent on the phenyl ring of aryl carboxamide moiety at 2nd position of 6-amino-4,5,6,7-tetrhydrobenzo[d]thiazole play a key role in inhibiting the proliferation of leukemia cells. Compounds with ortho substitution showed poor activity and with meta and para substitution showed good activity.
机译：最近，我们报道了（S）-6-芳基脲/硫脲取代的-2-氨基-4,5,6,7-四氢苯并[d]噻唑衍生物作为有效的抗白血病药的作用。为了进一步阐明结构活性关系（SAR）对（S）-2,6-二氨基-4,5,6,7-四氢苯并[d]噻唑部分（一系列被2-芳酰胺取代的）的抗白血病活性的研究设计，合成了-（S）-6-氨基-4,5,6,7-四氢苯并[d]噻唑，并通过台盼蓝排除法3-（4,5-二甲基噻唑-2-）评估了它们的抗白血病活性yl）-2,5-二苯基四唑溴化物（MTT），乳酸脱氢酶（LDH）分析和细胞周期分析。结果表明，在6-氨基-4,5,6,7-四氢苯并[d]噻唑的2位上，芳基羧酰胺部分苯环上的取代基的位置，数量和庞大性在抑制其增殖中起关键作用。白血病细胞。具有邻位取代的化合物显示出较差的活性，而具有间位和对位取代的化合物显示出了良好的活性。

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