HO-激活型核苷的区域选择性合成及抗癌活性评价。
Regioselective synthesis and anticancer evaluation of HO-activable nucleosides.
机构信息
Beijing National Laboratory for Molecular Sciences (BNLMS), CAS Key Laboratory of Molecular Recognition and Function, CAS Research/Education Center for Excellence in Molecular Sciences, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China.
出版信息
Chem Commun (Camb). 2020 Jun 16;56(48):6484-6487. doi: 10.1039/d0cc02245d.
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.
我们在这里描述了通过对非保护前体的高效和区域选择性功能化来设计、合成和生物评估 H2O2 激活的核苷。对吉西他滨的 H2O2 特异性响应前药的生物学评估表明，在两种细胞系中，其具有极快的激活作用、低毒性和增强的抗癌效果。
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