Cs2CO3-促进了3--2-1H的化:抗癌评估和分子对接
Kevin Salamanca-Perdigón1, Diana Hurtado-Rodríguez1, Jaime Portilla2
1Escuela de Ciencias Químicas, Universidad Pedagógica y Tecnológica de Colombia, Tunja, 150003, Colombia.
这项研究详细介绍了使用碳酸产生N--2-pyridones的3-cyano-2(1H) -pyridones的N-化. 一些O-alkylpyridine衍生物对A-498癌细胞表现出显著的选择性.
科学领域:
- 有机合成 有机合成
- 药品化学 药品化学 是一个
背景情况:
- 对于合成生物活性化合物而言,2-皮里顿的N-化是至关重要的.
- 化反应中的区域选择性受电子和硬质因素的影响.
研究的目的:
- 开发一个区域选择性N-化方法,用于3-cyano-2(1H) -pyridones.
- 为了进一步探索合成的N--2-pyridones的功能化.
- 为了评估O-酸衍生物的抗癌潜力.
主要方法:
- 由碳酸促进的3 - - 2 (((1H) - 化与基化的N-化.
- 铜 (I) 催化酸循环添加 (CuAAC) 用于三醇合成.
- (IV) 异氧化物催化的阿米达反应.
- 在体外针对A-498癌细胞系的抗癌活性查.
- 针对PIM-1激酶的分子对接研究.
主要成果:
- 实现了N--2-pyridones的高效合成,其区域选择性受环置换剂的影响.
- 用二甲基化物化导致复杂的产品混合物.
- N-基-2-pyridones被成功地功能化成1,2,3-triazoles和胺基.
- 甲基胺10b和10d对A-498细胞显著抑制了生长 (%GI为54.75和67.64).
结论:
- 一种Cs2CO3促进的N-化策略提供了一条可行的N--2-pyridones的途径.
- 合成的O-基二烯显示出有前途的抗癌活性,需要进一步研究.
- 分子对接表明与PIM-1激酶的潜在相互作用作为一种可能的作用机制.
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