Synthesis and antitumor activity of some nitrogen heterocycles bearing pyrimidine moiety,Journal of Heterocyclic Chemistry

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Synthesis and antitumor activity of some nitrogen heterocycles bearing pyrimidine moiety
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-07-19 , DOI: 10.1002/jhet.4061
Marwa H. Ahmed ₁ , Maher A. El‐Hashash ₁ , Magda I. Marzouk ₁ , Abeer M. El‐Naggar ₁

Affiliation

Synthesis of novel pyrimidine derivatives 4‐16 was accomplished by heterocyclization of polarized system, for example, Chalcone. Claisen‐Schmidt condensation of 2‐acetyl naphthalene with 4‐(N, N‐dimethylaminobenzaldehyde) afforded chalcone 3, which was utilized for synthesis various pyrimidine derivatives by treatment with urea, thiourea, and guandine hydrochloride in ethanolic sodium hydroxide solution. The reactivity of the synthesized pyrimidine derivatives towards different nucleophilic and electrophilic reagent were examined. The constructions of the newly synthesized pyrimidine derivatives were elucidated from their spectral and elemental analysis. All the synthesized compounds were tested in vitro for their anticancer activities against HePG‐2 and MCF‐7 cell lines. Some of them posses a wide range of pharmacological activity. Finally, a molecular docking study was conducted to reveal the probable interaction with the dihydrofolate reductase (DHFR) active site.

中文翻译：

一些带有嘧啶部分的氮杂环的合成及抗肿瘤活性

新型嘧啶衍生物4-16的合成是通过极化系统（如查尔酮）的杂环化完成的。2-乙酰基萘与4-（N，N-二甲基氨基苯甲醛）的Claisen-Schmidt缩合得到查耳酮3通过在乙醇氢氧化钠溶液中用尿素，硫脲和盐酸胍处理来合成各种嘧啶衍生物。检查了合成的嘧啶衍生物对不同亲核试剂和亲电试剂的反应性。从其光谱和元素分析中阐明了新合成的嘧啶衍生物的结构。所有合成的化合物均在体外测试了对HePG-2和MCF-7细胞系的抗癌活性。其中一些具有广泛的药理活性。最后，进行了分子对接研究以揭示与二氢叶酸还原酶（DHFR）活性位点的可能相互作用。

更新日期：2020-09-08

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