...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine >Synthesis of 11C-labeled Kendine 91, a histone deacetylase inhibitor
【24h】

Synthesis of 11C-labeled Kendine 91, a histone deacetylase inhibitor

机译：组蛋白脱乙酰基酶抑制剂11C标记的Kendine 91的合成

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

In the present paper, the synthesis of 11C-labeled Kendine 91 (a HDAC inhibitor which has shown in vitro and in vivo activity in HCT 116 and MOLT 4 human cancer cell lines) is described for the first time. The radiosynthesis has been approached by reaction of the non-radioactive precursor 6-((3-(4-hydroxyphenyl)-5-phenyl-1H-pyrrole-2-carboxamide))hexanehydroxamic acid with [ 11C]CH 3I in basic media. Despite the presence of more than one reactive site in the chemical structure of the precursor, acceptable radiochemical yield (8.2±2.1%, decay corrected to the end of bombardment), specific activity (28.2±9.4GBq/μmol) and radiochemical purity values (95%) were obtained in reasonably short preparation times (~40min). Despite the moderate radiochemical yield, final radioactivity and radioactivity concentration values (1.8±0.3GBq and 180MBq/ml, respectively) should be sufficient for putative in vivo studies in animals.
机译：在本文中，首次描述了11C标记的Kendine 91（一种HDAC抑制剂，已在HCT 116和MOLT 4人类癌细胞系中显示了体外和体内活性）的合成。通过在碱性介质中使非放射性前体6-（（（3-（4-羟基苯基）-5-苯基-1H-吡咯-2-羧酰胺））己烷异羟肟酸与[11C] CH 3I反应来进行放射性合成。尽管前驱体的化学结构中存在一个以上的反应位点，但可接受的放射化学收率（8.2±2.1％，衰减校正至轰击结束），比活（28.2±9.4GBq /μmol）和放射化学纯度值（ > 95％）是在相当短的准备时间内（〜40min）获得的。尽管放射化学产量适中，但最终的放射性和放射性浓度值（分别为1.8±0.3GBq和180MBq / ml）应足以进行动物体内研究。

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