Litcius/Paper detail

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

Ali H. Abu Almaaty, Eslam E. M. Toson, Elsherbiny H. El‐Sayed, Mohamed A. Tantawy, Eman Fayad, Ola A. Abu Ali, Islam Zaki

2021Molecules20 citationsDOIOpen Access PDF

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.

Topics & Concepts

ImidazoleChemistryErlotinibApoptosisCell cultureIn vitroCytotoxic T cellStereochemistryArylCytotoxicityCell cycleCancer cell linesCell cycle checkpointCarbon-13 NMRProton NMRCancer cellCancerBiochemistryBiologyAlkylReceptorEpidermal growth factor receptorOrganic chemistryGeneticsSynthesis and Characterization of Heterocyclic CompoundsSynthesis and biological activitySynthesis of heterocyclic compounds