SuFEx 点击化学启用后期药物功能化
Zilei Liu1,2, Jie Li1,2, Suhua Li2
1Department of Molecular Medicine, The Scripps Research Institute , La Jolla, California 92037, United States.
Journal of the American Chemical Society
|February 17, 2018
概括
硫交换 (SuFEx) 基因化学可以快速合成新型抗癌药物. 这种新方法快速生成和测试酸, 揭示了对癌细胞有更强效的化合物.
科学领域:
- 医学化学
- 有机化学
- 药物发现
背景情况:
- 硫交换 (SuFEx) 是一种新兴的点击化学技术.
- SuFEx化学为合成新型化合物提供了一个多功能平台.
- 它在药物发现中的应用还未得到充分研究.
研究的目的:
- 开发和验证一个在现场的方法,用于SuFEx化学在96井板.
- 为了快速合成和生物查酸衍生物.
- 探索SuFEx在抗癌药物晚期功能化的潜力.
主要方法:
- 在现场开发了SuFEx反应,用于将转化为硫酸盐.
- 使用自动合成和选来快速评估生物活性.
- 已知抗癌药物的晚期功能化.
主要成果:
- 鉴定了三种具有改善抗癌细胞增殖活性的酸.
- 硫酸衍生物在ER+乳腺癌细胞中表现出增强的活性.
- 抗药性结肠癌细胞的功效增加了70倍.
结论:
- 在现场开发的SuFEx方法与自动合成和选兼容.
- 这种方法有助于发现具有增强治疗功能的新药候选药物.
- 在加速药物发现和开发方面,
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