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Synthesis of some novel 2-(3-cyano -6-(thiophen- 2-yl)-4,4'- bipyridin-2- yloxy)acetohydrazide derivatives: assessment of their cytotoxic activity.
BMC Chemistry ( IF 4.6 ) Pub Date : 2020-06-02 , DOI: 10.1186/s13065-020-00692-4
Hossa F Al Shareef 1
Affiliation  

A new series of pyrazole, bipyridine, N-amide derivatives and Schiff bases was synthesized using compound 2-(3-cyano-6- (thiophen-2-yl)-4,4′- bipyridin-2-yloxy) acetohydrazide (3) as a starting material. The compounds structures were confirmed depending on the spectroscopic methods and elemental analysis. Also, the compounds were evaluated as anticancer agents by the compounds screened towards adenocarcinoma breast cancer cell line (MCF-7). The compounds showed a promising cytotoxic effect against human breast cancer cells. Compound 7c showed the most effective activity compared to other compounds with (IC50 = 0.6 ± 0.01 μg mL−1) in comparison with the reference drug doxorubicin (IC50 = 1.6 ± 0.02 μg mL−1). While compound 3 is closely active with doxorubicin. Also compounds 2, 4, 6, 7a, 7b and 7d showed noticeable cytotoxic effect. Early and late apoptotic cells were detected using Acridine orange/Ethidium bromide staining technique. The results of biologically screening of the tested compounds give an idea about the importance in the compounds acting against breast cancer and may lead to the discovery of a potent anticancer agent.

中文翻译:

一些新型的2-(3-氰基-6-(噻吩-2-基)-4,4'-联吡啶-2-基氧基)乙酰肼衍生物的合成:评估其细胞毒性活性。

使用化合物2-(3-氰基-6-(噻吩-2-基)-4,4'-联吡啶-2-基氧基)乙酰肼合成了一系列新的吡唑,联吡啶,N-酰胺衍生物和席夫碱)作为起始材料。根据光谱方法和元素分析确定化合物的结构。而且,通过针对腺癌乳腺癌细胞系(MCF-7)筛选的化合物,将该化合物评价为抗癌剂。这些化合物对人乳腺癌细胞显示出有希望的细胞毒性作用。与其他化合物(IC50 = 0.6±0.01μgmL-1)相比,化合物7c与其他化合物(IC50 = 1.6±0.02μgmL-1)相比,显示出最有效的活性。而化合物3与阿霉素密切相关。化合物2、4、6、7a,7b和7d也显示出明显的细胞毒性作用。使用A啶橙/溴乙锭染色技术检测早期和晚期凋亡细胞。对被测化合物进行生物学筛选的结果使人们对化合物在对抗乳腺癌中的重要性有了一个认识,并可能导致发现一种有效的抗癌剂。
更新日期:2020-06-02
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