5-Aryl-1-Arylideneamino-1H-Imidazole-2(3H)-Thiones: Synthesis and in Vitro Anticancer Evaluation

Molecules

EmanFayad¹  Ola A.Abu Ali²  El-SherbinyH.El-Sayed³  Eslam E. M. Toson³  MohamedA. M.Tantawy⁴  Islam Zaki⁵  Ali H. Abu Almaaty⁶ 

[1] . Biotechnology Department, Faculty of Science, Taif University, P.O. Box 11099, Taif 21944, Saudi Arabia;. Chemistry Department, College of Science, Taif University, P.O.Box 11099 Taif 21944, Saudi Arabia;. Chemistry Department, Faculty of Science, Port Said University, Port Said 42526, Egypt;. Medical Research Division, National Research Centre, Dokki, Giza 12511, Egypt;. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Port Said University, Port Said 42526, Egypt;. Zoology Department, Faculty of Science, Port Said University, Port Said 42526, Egypt;

关键词: imidazole;    synthesis;    cytotoxicity;    apoptosis;    cell cycle analysis;    Annexin V;   

DOI  :  10.3390/molecules26061706

来源: DOAJ

【 摘 要 】

A novel series of N-1 arylidene amino imidazole-2-thiones were synthesized, identified using IR, ¹H-NMR, and ¹³C-NMR spectral data. Cytotoxic effect of the prepared compounds was carried out utilizing three cancer cell lines; MCF-7 breast cancer, HepG2 liver cancer, and HCT-116 colon cancer cell lines. Imidazole derivative 5 was the most potent of all against three cell lines. DNA flow cytometric analysis showed that, imidazoles 4d and 5 exhibit pre-G1 apoptosis and cell cycle arrest at G2/M phase. The results of the VEGFR-2 and B-Raf kinase inhibition assay revealed that compounds 4d and 5 displayed good inhibitory activity compared with reference drug erlotinib.

【 授权许可】

Unknown