Rashdan Huda R M, Shehadi Ihsan A, Abdelmonsef Abobakr H
Chemistry of Natural and Microbial Products Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, Cairo 12622, Egypt.
Chemistry Department, Faculty of Science, University of Sharjah, Sharjah 27272, UAE.
ACS Omega. 2021 Jan 5;6(2):1445-1455. doi: 10.1021/acsomega.0c05116. eCollection 2021 Jan 19.
A novel series of 1,2,3-triazolyl-pyridine hybrids were prepared through the reaction of the triazole derivative () with the appropriate aldehyde () and malononitrile or ethyl cyanoacetate in the presence of ammonium acetate in refluxed acetic acid. The chemical composition of the products was established on the basis of spectral and elemental analyses. Aurora B kinase is a protein with diverse biological actions in controlling tumorigenesis by inhibiting apoptosis and promoting proliferation and metastasis, making it an emerging target for diseases such as hepatocellular carcinoma (HCC). Alteration in the target protein expression causes unequal distribution of genetic information, causing HCC. The new compounds were tested for their antihepatic cancer activity, and some of them had strong efficacy against human hepatoblastoma (HepG2) cell lines.
通过使三唑衍生物（）与适当的醛（）以及丙二腈或氰基乙酸乙酯在乙酸铵存在下于回流的乙酸中反应，制备了一系列新型的1,2,3 - 三唑基吡啶杂化物。产物的化学组成通过光谱和元素分析确定。Aurora B激酶是一种在通过抑制细胞凋亡以及促进增殖和转移来控制肿瘤发生过程中具有多种生物学作用的蛋白质，使其成为诸如肝细胞癌（HCC）等疾病的新兴靶点。靶蛋白表达的改变会导致遗传信息分布不均，从而引发HCC。对新化合物进行了抗肝癌活性测试，其中一些对人肝癌细胞系（HepG2）具有强效。
