Letters in Drug Design & Discovery ( IF 1.2 ) Pub Date : 2019-05-01 , DOI: 10.2174/1570180815666180816124102 Bedia Kocyigit-Kaymakcioglu 1 , Senem Sinem Yazici 1 , Fatih Tok 1 , Miriş Dikmen 2 , Selin Engür 2 , Emine Elçin Oruc-Emre 3 , Aysegul Iyidogan 3
Background: Hydrazones, one of the important classes of organic molecules, are pharmaceutical agents comprising –CO-NH-N=CH- group in the structure therefore and exhibiting significant biological activity.
Methods: 5-Chloro-N’-[(substituted)methylidene] pyrazine-2-carbohydrazide (3a-g) and their Pd(II) complexes (4a-h) were synthesized and investigated in vitro anticancer activity on A549, Caco2 cancer and normal 3T3 fibroblast cell lines, using the MTT assay.
Results: Anticancer activity screening results revealed that some compounds showed remarkable cytotoxic effect. Among them, 5-chloro-N'-[(4-hydroxyphenyl)methylidene] pyrazine-2-carbohydrazide (3c) displayed higher cytotoxic activity against A549 cancer cell line than the reference drug cisplatin.
Conclusion: Compound 3c showed high cytotoxic activity against A549 cancer cell line but it showed low cytotoxic effect against normal 3T3 fibroblast cell line. Antiproliferative and antimetastatic effects of 3c were determined by the real-time monitoring of cell proliferative system (RTCA DP). The cell proliferation, metastatic and invasive activities of A549 cells were decreased due to increased concentration of 3c.
中文翻译:
新型肼ide及其Pd(II)配合物的合成及抗癌活性
背景:,是重要的有机分子类别之一,是在结构中包含–CO-NH-N = CH-基团并具有显着生物学活性的药物。
方法:合成了5-氯-N'-[(取代)亚甲基]吡嗪-2-碳酰肼(3a-g)及其Pd(II)配合物(4a-h),并研究了其对A549,Caco2癌症的体外抗癌活性。 MTT法检测正常的3T3成纤维细胞系。
结果:抗癌活性筛选结果表明某些化合物具有显着的细胞毒性作用。其中,5-氯-N'-[(4-羟基苯基)亚甲基]吡嗪-2-碳酰肼(3c)对A549癌细胞系的细胞毒活性高于参考药物顺铂。
结论:化合物3c对A549癌细胞具有较高的细胞毒性,但对正常的3T3成纤维细胞具有较低的细胞毒性。通过实时监测细胞增殖系统(RTCA DP)来确定3c的抗增殖和抗转移作用。由于3c的浓度增加,A549细胞的细胞增殖,转移和侵袭活性降低。