作为潜在的抗癌剂的Diorganotin (IV) 氨基酸复合物. 合成,结构特征和体外检测分析
A Verónica Rodriguez-Mayor1, Ma Eugenia Ochoa1, Mónica Farfán-Paredes1
1Departamento de Química, Centro de Investigación y de Estudios Avanzados del IPN, Av, Instituto Politécnico Nacional 2508, Col. San Pedro Zacatenco, Gustavo A. Madero, C.P. 07360 Ciudad de México, México.
Journal of inorganic biochemistry
|May 21, 2024
概括
从L-氨基酸中提取的9种新型有机蛋白化合物被合成和特征化. 这些化合物对人类癌症细胞系表现出选择性的抗增殖活性,显示出作为化疗替代品的前景.
科学领域:
- 有机金属化学 有机金属化学
- 药用化学 医学化学
- 材料科学 材料科学 材料科学
背景情况:
- 有机蛋白化合物具有多样化的应用,包括在医学中.
- L-氨基酸为合成新型金属复合体提供了性构建块.
- 开发具有提高选择性的新抗癌药物是一个关键需求.
研究的目的:
- 使用L-氨基酸合成和表征新型有机素 (IV) 衍生物.
- 为了研究这些新化合物的结构性质.
- 评估它们作为抗癌剂的潜力.
主要方法:
- 一超声波辅助合成九种有机素 (IV) 衍生物.
- 使用ATR-FTIR,LRMS和溶液NMR (1H,13C,119Sn) 进行表征.
- 通过单晶X射线衍射对精选复合体进行结构阐明.
- 在Silico ADME使用SWISS ADME进行物业预测.
- 在体外对人类癌细胞系 (HT-29,MDA-MB-231,SW-1353) 和对照细胞系进行抗增殖活性测试.
主要成果:
- 成功合成并对九种有机素 (IV) -L-氨基酸衍生物进行了完整的鉴定.
- X射线衍射揭示了不同的固态结构:五个协调的单核物种和六个协调的聚合物网络.
- 溶液NMR证实了溶液中的五协调单核物种.
- ADME的预测表明了有利的药理动力学特征.
- 对测试的癌细胞系表现出选择性抗增殖活性,对非瘤细胞的影响最小.
结论:
- 合成的有机素 (IV) 衍生物具有独特的结构特征和有利的预测ADME特性.
- 这些化合物具有显著的选择性抗癌活性,表明它们作为新型治疗剂的潜力.
- 对这些有机蛋白复合物的进一步研究可能会导致新的化疗替代方案.
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