Nikolova-Mladenova Boriana, Halachev Nenko, Iankova Rumjana, Momekov Georgi, Ivanov Darvin
Department of Chemistry, Faculty of Pharmacy, Medical University, Sofia, Bulgaria.
Arzneimittelforschung. 2011;61(12):714-8. doi: 10.1055/s-0031-1300592.
Three new hydrazones, derivatives of salicylaldehyde benzoylhydrazone, were synthesized as potential anti-proliferative compounds. The structure of the new compounds was characterized by elemental and thermo-gravimetric analyses, IR, 1H and 13C-NMR spectroscopy and quantum chemical calculations. The cytotoxic effects of new hydrazones were examined on a wide spectrum of human tumor cell lines. The obtained results revealed that all compounds proved to be equipotent or moreactive than cisplatin, and far more activethan another utilized anticancer drug, melphalan. On the basis of IC50 values the compound 3-methoxy-salicylaldehyde isonicotinoylhydrazone (mSIH) was found to be the most active cytotoxic agent at all cell lines.
合成了三种新型腙，即水杨醛苯甲酰腙衍生物，作为潜在的抗增殖化合物。通过元素分析、热重分析、红外光谱、1H和13C核磁共振光谱以及量子化学计算对新化合物的结构进行了表征。研究了新型腙对多种人类肿瘤细胞系的细胞毒性作用。所得结果表明，所有化合物均被证明与顺铂具有同等效力或更具活性，且比另一种使用的抗癌药物美法仑活性高得多。根据IC50值，发现化合物3-甲氧基水杨醛异烟酰腙（mSIH）在所有细胞系中是最具活性的细胞毒性剂。
