新型腙衍生物的合成及其作为人癌细胞增殖抑制剂的功效评价。
Synthesis of New Hydrazone Derivatives and Evaluation of their Efficacy as Proliferation Inhibitors in Human Cancer Cells.
机构信息
Department of Chemistry of Drugs, Wroclaw Medical University, Borowska 211, 50-556 Wroclaw, Poland.
Department of Molecular and Cellular Biology, Wroclaw Medical University, Borowska 211A, 50-556 Wroclaw, Poland.
出版信息
Med Chem. 2019;15(8):903-910. doi: 10.2174/1573406415666190128100524.
BACKGROUND
Hydrazine-hydrazones represent a group of bioactive compounds that display antibacterial, anti-inflammatory, antiviral or anticancer activities.
OBJECTIVE
In this study, we designed new derivative compounds from groups of hydrazones.
METHODS
The group of new derivatives was evaluated by the viability assay in human cancer and normal cells.
RESULTS
The dimethylpyridine hydrazones showed potent inhibition of cell proliferation of breast, colon cancer cells, human melanoma and glioblastoma. Compound 12 inhibited proliferation of cancer cells exhibiting a drug-resistant phenotype (MCF-7/DX and LoVoDX) at low millimolar concentrations. Whereas, antimelanoma activity was revealed by Compounds 2, 4, 7 and 12.
CONCLUSION
The present results highlighted newly synthetized hydrazine derivatives an excellent base for the design of new anticancer agents and resistance inhibitors.
背景
水合肼腙类化合物具有抗菌、抗炎、抗病毒或抗癌活性，是一组具有生物活性的化合物。
目的
在这项研究中，我们设计了新的腙类衍生物。
方法
通过人癌细胞和正常细胞的活力测定评估新衍生物组。
结果
二甲基吡啶腙类化合物对乳腺癌、结肠癌、人黑色素瘤和神经胶质瘤细胞的增殖具有很强的抑制作用。化合物 12 以低毫摩尔浓度抑制表现出耐药表型（MCF-7/DX 和 LoVoDX）的癌细胞增殖。然而，化合物 2、4、7 和 12 显示出抗黑色素瘤活性。
结论
本研究结果强调了新合成的水合肼衍生物是设计新型抗癌药物和耐药抑制剂的极好基础。
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