Fluorescent anticancer quinazolines as molecular probes for β-tubulin colchicine site competition assay and visualization of microtubules as intracellular targeting sites
Fluorescent anticancer quinazolines as molecular probes for β-tubulin colchicine site competition assay and visualization of microtubules as intracellular targeting sites
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DOI：
10.1016/j.dyepig.2017.05.050
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发表时间：
2017-10-01
影响因子：
4.5
通讯作者：
Asai, Akira
中科院分区：
文献类型：
--
作者：
Suzuki, Yumiko;Sawada, Jun-ichi;Asai, Akira
抗癌2-氨基喹唑啉类化合物的物理化学性质进行了评估，响应媒体的变化。通过与β-微管蛋白的秋水仙碱结合位点结合，2-N-吗啉代衍生物（1）的荧光发射蓝移，强度增强。这些杰出的功能被用于开发的β-微管蛋白秋水仙碱位点竞争试验和可视化的细胞内分布的1通过荧光显微镜。
Anticancer 2-aminoquinazolines were evaluated by their photophysical properties responding to media changes. By binding to the colchicine binding site of beta-tubulin, the fluorescence emission of 2-N-morpholino-derivative (1) was blue-shifted with enhanced intensity. These distinguished features were used for the development of a beta-tubulin colchicine site competition assay and visualization of the intracellular distribution of 1 by fluorescence microscopy.