Green synthesis of 1,3,4‐oxadiazole derivatives based on N‐arylidene‐2‐(1‐oxo‐4‐(4‐phenoxyphenyl)phthalazin‐2(1H)‐yl)acetohydrazide as potential antitumor agents,Journal of Heterocyclic Chemistry

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Green synthesis of 1,3,4‐oxadiazole derivatives based on N‐arylidene‐2‐(1‐oxo‐4‐(4‐phenoxyphenyl)phthalazin‐2(1H)‐yl)acetohydrazide as potential antitumor agents
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-11-03 , DOI: 10.1002/jhet.4181
Mohamed S. Behalo ₁ , Ebtsam S. El Said ₁

Affiliation

Design of a new series of 1,3,4‐oxadiazole derivatives was achieved in good yield via treatment of N‐arylidene‐2‐(1‐oxo‐4‐(4‐phenoxyphenyl)phthalazin‐2(1H)‐yl)acetohydrazide with cerium (IV) ammonium nitrate as a catalyst. They can be formulated also using one‐pot reaction of 2‐(1‐oxo‐4‐(4‐phenoxyphenyl)phthalazin‐2(1H)‐yl)acetohydrazide, aromatic aldehyde and cerium (IV) ammonium nitrate in dichloromethane. The structural formulas of all synthesized products were elucidated based on their elemental and spectral analyses. In addition, MTT assay was used to evaluate antitumor activity of the synthesized molecules and some of them showed potent activity in comparison with Doxorubicin as a standard drug.

中文翻译：

基于N-亚芳基-2-（1-氧代-4-（4-苯氧基苯基）酞嗪-2（1H）-基）乙酰肼作为潜在抗肿瘤剂的1,3,4-恶二唑衍生物的绿色合成

通过处理N-亚芳基-2-（1-氧代-4-（4-苯氧基苯基）酞嗪-2-（1 H）-基），以高收率设计了一系列新的1,3,4-恶二唑衍生物。乙酰肼，以硝酸铈（四）铵为催化剂。也可以使用二氯甲烷中的2-（1-氧--4-（4-苯氧基苯基）酞嗪-2（1 H）-基）乙酰肼，芳族醛和硝酸铈（IV）铵的一锅反应来配制它们。根据元素分析和光谱分析，阐明了所有合成产物的结构式。另外，MTT测定法用于评估合成分子的抗肿瘤活性，并且与阿霉素作为标准药物相比，其中一些显示出有效的活性。

更新日期：2020-11-03

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