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Synthesis and Biological Activity of New Diazenedicarboxamides as Potential Anticancer Agents

机译:新型二氮杂二羧酸酰胺类化合物的合成及其生物活性

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To increase the effectiveness of cancer treatment, more effective anti-cancer drugs, as well as the new improved strategies of cancer treatment, are urgently needed. Our previous results have shown that various diazenes are cytotoxic to different tumor cells and can even revert the resistance to cisplatin and vincristine. We also demonstrated that unsymmetri-cal diazenedicarboxamides 1 and 2 exhibited promising cytotoxicity. The aim of the present study was to synthesize new diazenedicarboxamides with acceptable solubility and good cytotoxicity. Here we report the synthesis and biological evaluation of new N,N'-disubstituted diazenedicarboxamides. We found that a modification of either 1 or 2 led to the more active compounds. The most effective among them was diazenedicarboxamide 11, which can be considered as a new potential anticancer agent for the tumors of different origin, as well as for the drug resistant tumors.
机译:为了提高癌症治疗的有效性,迫切需要更有效的抗癌药物以及新的改良的癌症治疗策略。我们以前的结果表明,不同的二氮嗪对不同的肿瘤细胞具有细胞毒性,甚至可以恢复对顺铂和长春新碱的耐药性。我们还证明了不对称的二氮杂二羧酰胺1和2表现出有希望的细胞毒性。本研究的目的是合成具有可接受的溶解度和良好的细胞毒性的新的二氮杂二羧酰胺。在这里,我们报告了新的N,N'-二取代的二氮杂二烷基羧酰胺的合成和生物学评估。我们发现1或2的修饰导致活性更高的化合物。其中最有效的是二氮杂双羧酰胺11,可以将其视为针对不同来源的肿瘤以及耐药性肿瘤的新型潜在抗癌药。

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