Abstract
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.
Highlights
The results showed that the selected candidates induce apoptosis of MCF-7 cells at both early and later stages
The results proved that the antiproliferative activity of compounds 4d and 5 is attributed to its apoptosis inducing activity in MCF-7 cells
A novel series of imidazoles bearing arylidene amino substituents at the N-1 position were synthesized in order to investigate their anticancer activity
Summary
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. Imidazoles are an important class of heterocyclic molecules and imidazole derivatives are reported to have anticancer activity [6,7,8]. Lepidiline A and B are imidazole compounds which exhibit cytotoxicity against various types of human cancer cell lines at micromolar concentration [11]. Imidazole derivatives were found to exert their anticancer activity by acting mainly as antiangiogenic agents, inhibitors of B-Raf kinase, and as p38 MAP kinase inhibitors [12,13,14]. Compound III displayed potent antitumor activity against the MCF-7 cell line with an IC50 value of 3.26 μM, as compared with SOR (IC50 = 1.12 μM) [15]. It has been reported that imidazole molecule V inhibits the kinase activity of Raf in low nanomolecular concentrations [16]. Full details about the synthesis and evaluation of the antitumor activity in vitro are reported
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
