• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Chemistry: A European journal >Preparation of Thermocleavable Conjugates Based on Ansamitocin and Superparamagnetic Nanostructured Particles by a Chemobiosynthetic Approach
【24h】

Preparation of Thermocleavable Conjugates Based on Ansamitocin and Superparamagnetic Nanostructured Particles by a Chemobiosynthetic Approach

机译：化学合成方法制备基于安托霉素和超顺磁性纳米结构粒子的热裂解结合物

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

A combination of mutasynthesis, precursor-directed biosynthesis and semisynthesis provides access to new ansamitocin derivatives including new nanostructured particle-drug conjugates. These conjugates are based on the toxin ansamitocin and superparamagnetic iron oxide-silica core shell particles. New ansamitocin derivatives that are functionalized either with alkynyl- or azido groups in the ester side chain at C-3 are attached to nanostructured iron oxide core-silica shell particles. Upon exposure to an oscillating electromagnetic field these conjugates heat up and the ansamitocin derivatives are released by a retro-Diels-Alder reaction. For example, one ansamitocin derivative exerts strong antiproliferative activity against various cancer cell lines in the lower nanomolar range while the corresponding nanostructured particle-drug conjugate is not toxic. Therefore, these new conjugates can serve as dormant toxins that can be employed simultaneously in hyperthermia and chemotherapy when external inductive heating is applied.
机译：突变合成，前体定向生物合成和半合成的结合提供了获得新的安索霉素衍生物的途径，包括新的纳米结构的颗粒-药物缀合物。这些结合物基于毒素安托霉素和超顺磁性氧化铁-二氧化硅核壳颗粒。在C-3的酯侧链中被炔基或叠氮基官能化的新的安托霉素衍生物与纳米结构的氧化铁核-二氧化硅壳颗粒相连。一旦暴露于振荡电磁场，这些结合物就会加热，而安那霉素衍生物会通过逆Diels-Alder反应释放。例如，一种安那霉素衍生物在较低的纳摩尔范围内对各种癌细胞系表现出强的抗增殖活性，而相应的纳米结构的颗粒-药物结合物则无毒。因此，这些新的结合物可以用作休眠毒素，当应用外部感应加热时，可以同时用于热疗和化疗中。

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