Department of Medical Biotechnology, Genetic Engineering & Biotechnology Research Institute (GEBRI), City of Scientific Research & Technological Applications (SRTA-city), Borg El-Arab, Alexandria, Egypt.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alexandria University, Alexandria 21521, Egypt.
Future Med Chem. 2019 Jul;11(13):1583-1603. doi: 10.4155/fmc-2018-0285.
Cyclooxygenase-2 (COX-2) inhibition and scavenging-free radicals are important targets in cancer treatment. Sulfanylpyrimidines and triazolopyrimidines were synthesized and evaluated as anticancer and antioxidant COX-1/2 inhibitors. Compound showed the same growth inhibitory activity as 5-fluorouracil against MCF-7. Compound displayed broad-spectrum anticancer activity against the four tested cancer cell lines. Compounds and were found to be more active antioxidants than trolox. Compounds and revealed high COX-2 inhibitory activity and selectivity, which was confirmed by docking studies. Compound could be considered as promising anticancer and antioxidant structural lead with COX-2 inhibition that deserve further derivatization and investigation.
环氧化酶-2（COX-2）抑制和清除自由基是癌症治疗的重要靶点。合成了巯基嘧啶和三唑嘧啶，并将其评估为抗癌和抗氧化 COX-1/2 抑制剂。化合物 对 MCF-7 的生长抑制活性与 5-氟尿嘧啶相同。化合物 对四种测试的癌细胞系显示出广谱抗癌活性。发现化合物 和 比 trolox 更具有活性抗氧化剂。化合物 和 表现出高 COX-2 抑制活性和选择性，这通过对接研究得到了证实。化合物 可以被认为是具有 COX-2 抑制作用的有前途的抗癌和抗氧化结构先导化合物，值得进一步衍生和研究。
