Regioselective synthesis and anticancer evaluation of H2O2-activable nucleosides

Regioselective synthesis and anticancer evaluation of H2O2-activable nucleosides
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H2O2激活核苷的区域选择性合成及抗癌评价

DOI:
10.1039/d0cc02245d
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发表时间:
2020
期刊:
Chem. Commun.
影响因子:
--
通讯作者:
Liang Cheng
Liang Cheng
中科院分区:
其他
文献类型:
--
作者:
Ying-Jie Sun;Li Liu;Liang Cheng

文献摘要

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我们在这里描述的设计,合成和生物评价的h2o2活化核苷通过一个有效的和区域选择性功能化无保护的前体。对吉美他滨h2o2特异性反应性前药的生物学评价表明,其在两种细胞系中具有极快的激活、低毒性和增强的抗癌作用。
We describe here the design, synthesis, and biological evaluation of H2O2-activatable nucleosides via an efficient and regioselective functionalization of unprotected precursors. Biological evaluation of a H2O2-specific responsive prodrug of gemecitabin demonstrates an extremely fast activation, low toxicity and enhanced anticancer effects in two cell lines.