New pyrimidines and triazolopyrimidines as antiproliferative and antioxidants with cyclooxygenase-1/2 inhibitory potential

Omar Ashraf M.; Abd El Razik Heba A.; Hazzaa Aly A.; El-Attar Maryam A. Z.; El Demellawy Maha A.; Wahab Abeer E. Abdel; El Hawash Soad A. M.

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New pyrimidines and triazolopyrimidines as antiproliferative and antioxidants with cyclooxygenase-1/2 inhibitory potential

机译：新的嘧啶和三唑基嘧啶作为抗增殖和抗氧化剂，环氧氧酶-1 / 2抑制潜力

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Cyclooxygenase-2 (COX-2) inhibition and scavenging-free radicals are important targets in cancer treatment. Materials & methods: Sulfanylpyrimidines and triazolopyrimidines were synthesized and evaluated as anticancer and antioxidant COX-1/2 inhibitors. Results: Compound 7 showed the same growth inhibitory activity as 5-fluorouracil against MCF-7. Compound 6f displayed broad-spectrum anticancer activity against the four tested cancer cell lines. Compounds 5b, 6a, 6c, 6d and 8 were found to be more active antioxidants than trolox. Compounds 6a, 6c, 6f and 8 revealed high COX-2 inhibitory activity and selectivity, which was confirmed by docking studies. Conclusion: Compound 6f could be considered as promising anticancer and antioxidant structural lead with COX-2 inhibition that deserve further derivatization and investigation.

机译：环氧氧基酶-2（COX-2）抑制和无清除的自由基是癌症治疗中的重要靶标。材料和方法：合成磺基吡啶和三唑嘧啶和三唑嘧啶，并评估为抗癌和抗氧化COX-1/2抑制剂。结果：化合物7显示出与MCF-7的5-氟尿嘧啶相同的生长抑制活性。化合物6F针对四种测试的癌细胞系显示广谱抗癌活性。发现化合物5b，6a，6c，6d和8是比擦油更具有更活跃的抗氧化剂。化合物6a，6c，6f和8显示了通过对接研究证实的高Cox-2抑制活性和选择性。结论：化合物6F可被认为是有前途的抗癌和抗氧化结构铅，COX-2抑制应该得到进一步的衍生化和调查。

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来源
《Future medicinal chemistry》 |2019年第13期|共21页
作者
Omar Ashraf M.; Abd El Razik Heba A.; Hazzaa Aly A.; El-Attar Maryam A. Z.; El Demellawy Maha A.; Wahab Abeer E. Abdel; El Hawash Soad A. M.;
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作者单位

City Sci Res &

Technol Applicat SRTA City Genet Engn &

Biotechnol Res Inst Dept Med Biotechnol;

Alexandria Univ Fac Pharm Dept Pharmaceut Chem Alexandria 21521 Egypt;

Alexandria Univ Fac Pharm Dept Pharmaceut Chem Alexandria 21521 Egypt;

Alexandria Univ Fac Pharm Dept Pharmaceut Chem Alexandria 21521 Egypt;

City Sci Res &

Technol Applicat SRTA City Genet Engn &

Biotechnol Res Inst Dept Med Biotechnol;

City Sci Res &

Technol Applicat SRTA City Genet Engn &

Biotechnol Res Inst Dept Med Biotechnol;

Alexandria Univ Fac Pharm Dept Pharmaceut Chem Alexandria 21521 Egypt;

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原文格式 PDF
正文语种 eng
中图分类药学;
关键词
anticancer; antioxidant; COX-1/2 inhibition; pyrimidines; triazolopyrimidines;

机译：抗癌;抗氧化剂;COX-1/2抑制;嘧啶;三唑嘧啶;

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1. New pyrimidines and triazolopyrimidines as antiproliferative and antioxidants with cyclooxygenase-1/2 inhibitory potential [J] . Omar Ashraf M., Abd El Razik Heba A., Hazzaa Aly A., Future medicinal chemistry . 2019,第13期

机译：新的嘧啶和三唑基嘧啶作为抗增殖和抗氧化剂，环氧氧酶-1 / 2抑制潜力
2. Biopotential of Bersama abyssinica Fresen Stem Bark Extracts: UHPLC Profiles, Antioxidant, Enzyme Inhibitory, and Antiproliferative Propensities [J] . Kouadio Ibrahime Sinan, Annalisa Chiavaroli, Giustino Orlando, Antioxidants . 2020,第2期

机译：Bersama Abyssinica Fresen Step Bark提取物的生物能妇：UHPLC型材，抗氧化剂，酶抑制和抗增殖性施力
3. New pyrazolo(3,4-d)pyrimidines endowed with A431 antiproliferative activity and inhibitory properties of Src phosphorylation. [J] . Schenone S, Bruno O, Ranise A, Bioorganic and Medicinal Chemistry Letters . 2004,第10期

机译：新的吡唑并（3,4-d）嘧啶具有A431的抗增殖活性和Src磷酸化的抑制特性。
4. Saponin, Polyphenol, Flavonoid content and α-gincosidase Inhibitory Activity, Antioxidant Potential of Launaea sarmentosa Leaves grown in Ben Tre province, Vietnam [C] . Le Thi Them, Phu Tuong Nguyen Dung, Pham Thi Nhat Trinh International Conference on Mechanical Engineering, Materials Science and Civil Engineering . 2019

机译：皂甙，多酚，黄酮类化酶抑制活性，Launaea Sarmentosa的抗氧化潜力在Ben Tre省生长，越南
5. The Inhibitory Effect of Natural Antioxidants on Formation of 2-amino-1-methyl-6-phenylimidazo [4, 5-b] Pyridine (PhIP) in a Model System [D] . Al-bashabsheh, Zaher. 2019

机译：天然抗氧化剂对模型系统中2-氨基-1-甲基-6-苯基咪唑[4,5-B]吡啶（PHIP）形成的抑制作用
6. Biopotential of Bersama abyssinica Fresen Stem Bark Extracts: UHPLC Profiles Antioxidant Enzyme Inhibitory and Antiproliferative Propensities [O] . Kouadio Ibrahime Sinan, Annalisa Chiavaroli, Giustino Orlando, 2020

机译：深层Bersama的Fresen干树皮提取物的生物潜力：UHPLC谱抗氧化剂酶抑制和抗增殖倾向
7. Biopotential of Bersama abyssinica Fresen Stem Bark Extracts: UHPLC Profiles, Antioxidant, Enzyme Inhibitory, and Antiproliferative Propensities [O] . Kouadio Ibrahime Sinan, Annalisa Chiavaroli, Giustino Orlando, 2020

机译：Bersama Abyssinica Fresen Step Bark提取物的生物能妇：UHPLC型材，抗氧化剂，酶抑制和抗增殖性施力

New pyrimidines and triazolopyrimidines as antiproliferative and antioxidants with cyclooxygenase-1/2 inhibitory potential

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