• 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 >Thiazolyl N-benzyl-substituted acetamide derivatives: synthesis, Src kinase inhibitory and anticancer activities.
【24h】

Thiazolyl N-benzyl-substituted acetamide derivatives: synthesis, Src kinase inhibitory and anticancer activities.

机译：噻唑基N-苄基取代的乙酰胺衍生物：合成，Src激酶抑制和抗癌活性。

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

KX2-391 (KX-01/Kinex Pharmaceuticals), N-benzyl-2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)acetamide, is a highly selective Src substrate binding site inhibitor. To understand better the role of pyridine ring and N-benzylsubstitution in KX2-391 and establish the structure-activity relationship, a number of N-benzyl substituted (((2-morpholinoethoxy)phenyl)thiazol-4-yl)acetamide derivatives containing thiazole instead of pyridine were synthesized and evaluated for Src kinase inhibitory activities. The unsubstituted N-benzyl derivative (8a) showed the inhibition of c-Src kinase with GI(50) values of 1.34 muM and 2.30 muM in NIH3T3/c-Src527F and SYF/c-Src527F cells, respectively. All the synthesized compounds were evaluated for inhibition of cell proliferation of human colon carcinoma (HT-29), breast carcinoma (BT-20), and leukemia (CCRF-CEM) cells. 4-Fluorobenzylthiazolyl derivative 8b exhibited 64-71% inhibition in the cell proliferation of BT-20 and CCRF cells at concentration of 50 muM.
机译：KX2-391（KX-01 / Kinex Pharmaceuticals）N-苄基-2-（5-（4-（2-吗啉代乙氧基）苯基）吡啶-2-基）乙酰胺是一种高度选择性的Src底物结合位点抑制剂。为了更好地了解吡啶环和N-苄基取代在KX2-391中的作用并建立结构-活性关系，许多含有噻唑的N-苄基取代的（（（2-吗啉代乙氧基）苯基）噻唑-4-基）乙酰胺衍生物合成吡啶而不是吡啶并评估Src激酶抑制活性。未取代的N-苄基衍生物（8a）在NIH3T3 / c-Src527F和SYF / c-Src527F细胞中的GI（50）值分别显示c-Src激酶的抑制作用为1.34μM和2.30μM。评价所有合成的化合物对人结肠癌（HT-29），乳腺癌（BT-20）和白血病（CCRF-CEM）细胞的细胞增殖的抑制作用。 4-氟苄基噻唑基衍生物8b在浓度为50μM时对BT-20和CCRF细胞的细胞增殖表现出64-71％的抑制作用。

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