Shaker Yasser M, Omar Mohamed A, Mahmoud Khaled, Elhallouty Salwa M, El-Senousy Waled M, Ali Mamdouh M, Mahmoud Abeer E, Abdel-Halim Abeer H, Soliman Saeed M, El Diwani Hoda I
a Department of Chemistry of Natural and Microbial Products .
J Enzyme Inhib Med Chem. 2015;30(5):826-45. doi: 10.3109/14756366.2014.979344.
A novel series of 5-nitro-1H-benzimidazole derivatives substituted at position 1 by heterocyclic rings was synthesized. Cytotoxicity and antiviral activity of the new compounds were tested. Compound 3 was more active than doxorubicin against A-549, HCT-116 and MCF-7. However, compound 3 showed no activity against human liver carcinoma Hep G-2 cell line. Compounds 9 and 17b (E) showed potency near to doxorubicin against the four cell lines. The acute toxicity of compound 9 on liver cancer induced in rats was determined in vivo. Interestingly, it showed restoration activity of liver function and pathology towards normal as compared to the cancer-bearing rats induced by DENA. Compounds 17a (Z), 17b (E) and 18a (Z) were the most promising compounds for their antiviral activity against rotavirus Wa strain.
合成了一系列新型的5-硝基-1H-苯并咪唑衍生物，其1位被杂环取代。测试了新化合物的细胞毒性和抗病毒活性。化合物3对A-549、HCT-116和MCF-7的活性比阿霉素更高。然而，化合物3对人肝癌Hep G-2细胞系无活性。化合物9和17b（E）对这四种细胞系显示出与阿霉素相近的效力。在体内测定了化合物9对大鼠诱发肝癌的急性毒性。有趣的是，与二乙基亚硝胺诱导的荷癌大鼠相比，它显示出肝功能和病理恢复至正常的活性。化合物17a（Z）、17b（E）和18a（Z）是对轮状病毒Wa株具有抗病毒活性的最有前景的化合物。
