达沙替尼
化学
DNA
结合
点击化学
组合化学
立体化学
生物化学
酪氨酸激酶
受体
数学
数学分析
作者
Nan Sheng Li,Nathan Gossai,Jordan A. Naumann,Peter M. Gordon,Joseph A. Piccirilli
标识
DOI:10.1021/acs.bioconjchem.6b00557
摘要
A pair of synthetic approaches to linear dasatinib–DNA conjugates via click chemistry are described. The first approach involves the reaction of excess azido dasatinib derivative with 5′-(5-hexynyl)-tagged DNAs, and the second involves the reaction of excess alkynyl-linked dasatinib with 5′-azido-tagged DNA. The second approach using alkynyl-derived dasatinib and 5′-azido-tagged DNA yielded the corresponding dasatinib-DNA conjugates in higher yield (47% versus 10–33% for the first approach). Studies have shown these linear dasatinib–DNA conjugates-derived gold nanoparticles exhibit efficacy against leukemia cancer cells with reduced toxicity toward normal cells compared to that of free dasatinib.
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