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Facile synthesis and anticancer activity of novel dihydropyrimidinone derivatives
Polish Journal of Chemical Technology ( IF 0.7 ) Pub Date : 2022-03-01 , DOI: 10.2478/pjct-2022-0004
Mashooq A. Bhat 1 , Mohamed A. Al-Omar 1 , Ahmed M. Naglah 1 , Abdullah Al-Dhfyan 2
Affiliation  

Abstract The enaminone, (2E)-3-(dimethylamino)-1-(3,4,5-trimethoxyphenyl) prop-2-en-1-one was prepared by refluxing 3,4,5-trimethoxy acetophenone with dimethylformamide dimethylacetal (DMF–DMA) without solvent for 12 h. The dihydropyrimidinone derivatives (1–9) were prepared by reacting enaminone, substituted benzaldehydes and urea in glacial acetic acid. The compounds (1–9) were synthesized in significant yield using one step multicomponent reaction. Structures of all the novel synthesized compounds were characterized and confirmed by various spectroscopic methods. The compounds were evaluated for their anti-cancer activity against HepG2 cancer cell line. Compound 9 displayed significant anti-cancer activity. During the apoptotic assay, it showed a significant increase in necrosis from 1.97% to 12.18% as compared to the control. Mechanism of anti-proliferation was performed by cell cycle distribution assay, which showed a decrease in G2+M from 12.90 to 8.13 as compared to control.

中文翻译:

新型二氢嘧啶酮衍生物的简便合成和抗癌活性

摘要 以 3,4,5-三甲氧基苯乙酮与二甲基甲酰胺二甲基缩醛( DMF-DMA) 无溶剂 12 小时。通过烯胺酮、取代的苯甲醛和尿素在冰醋酸中反应制备二氢嘧啶酮衍生物 (1-9)。使用一步多组分反应以显着收率合成化合物(1-9)。通过各种光谱方法对所有新合成化合物的结构进行了表征和确认。评估了这些化合物对 HepG2 癌细胞系的抗癌活性。化合物9显示出显着的抗癌活性。在细胞凋亡测定期间,与对照相比,它显示坏死从 1.97% 显着增加至 12.18%。
更新日期:2022-03-01
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