Graduate Institute of Life Science, National Defense Medical Center, No. 161, Sec. 6, Minquan E. Rd., Neihu Dist., Taipei City 11490, Taiwan, Republic of China.
Department of Physiology & Biophysics, National Defense Medical Center, No. 161, Sec. 6, Minquan E. Rd., Neihu Dist., Taipei City 11490, Taiwan, Republic of China.
Molecules. 2022 Apr 4;27(7):2325. doi: 10.3390/molecules27072325.
In this report, 19 boron-containing depsipeptides were synthesized via microwave-assisted Passerini three-component reaction (P-3CR) in an aqueous environment. The linker-free DAHMI fluorescent tagging approach was used on selected boron-containing compounds to study the relationship between their structures and their level of cellular uptake of HEK293 cells. The biological data retrieved from the DAHMI experiments indicated that while the structures of tested compounds may be highly similar, their bio-distribution profile could be vastly distinctive. The reported optimized one-pot synthetic strategy along the linker-free in vitro testing protocol could provide an efficient platform to accelerate the development of boron-containing drugs.
在本报告中，通过微波辅助的 Passerini 三组分反应（P-3CR）在水相环境中合成了 19 种含硼的 depsipeptides。在选定的含硼化合物上使用无连接子的 DAHMI 荧光标记方法研究了它们的结构与其在 HEK293 细胞中的摄取水平之间的关系。DAHMI 实验获得的生物学数据表明，尽管测试化合物的结构可能非常相似，但它们的生物分布情况可能有很大的差异。报告的优化的一锅合成策略以及无连接子的体外测试方案可以提供一个有效的平台来加速含硼药物的开发。
