新型特里亚佐洛皮里丁衍生物:合成,抗菌,抗癌评估和分子对接研究
Amina A Abd El-Gwaad1, Dina A Ali2, Hanem M Awad3
1Department of Therapeutic Chemistry, Pharmaceutical and Drug Industries Research Institute, National Research Centre, Cairo, Egypt.
新的三烯衍生物被合成并选用于抗微生物和抗癌性质. 化合物4和6对特定的癌症细胞系,特别是荷尔蒙依赖性乳腺癌和某些微生物表现出显著的活性.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 药理学 药理学是指药理学的学科.
背景情况:
- 三烯酸衍生物是一种具有多种生物活性的异环化合物.
- 开发具有强大的抗微生物和抗癌特性的新型化合物是研究的一个重要领域.
研究的目的:
- 设计,合成和评估新的三烯衍生物及其抗微生物和体外细胞毒性作用.
- 为特定的人类癌症细胞系识别选择性抗癌剂.
主要方法:
- 使用活性碳化合物,酸和化物合成新型三烯衍生物.
- 使用FT-IR,1H NMR,13C NMR和质谱学进行结构阐明.
- 通过磁盘扩散试验和体外细胞毒性评估对各种人类癌症和健康细胞系进行抗菌查.
主要成果:
- 化合物4,5,6和10对测试的微生物表现出显著的抗菌活性.
- 所有测试的化合物 (4-10) 对MCF-7 (荷尔蒙依赖性乳腺癌) 细胞系表现出高活性.
- 化合物4和6对MCF-7,HCT-116 (结肠癌) 和HepG2 (肝癌) 细胞系表现出选择性细胞毒性,对MDA-MB-231 (荷尔蒙独立乳腺癌) 没有活性.
结论:
- 合成的triazolopyridine衍生物作为潜在的抗菌剂具有前景.
- 化合物4和6被认为是治疗激素依赖性乳腺癌,结肠癌和肝癌的有希望的候选物,因为它们具有选择性细胞毒性作用.
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