Unveiling the Full Potential of 2-aryl-1H-phenanthro [9,10-d] imidazoles as Cytotoxic Agents vs AGS, HepG2 and MCF-7 Cell lines

Document Type : Research Article


1 Department of Chemistry, Ahvaz Branch, Islamic Azad University, Ahvaz, I.R. IRAN

2 Department of Pharmacology and Toxicology, School of Pharmacy, Ardabil University of Medical Sciences, Ardabil, I.R. IRAN

3 Department of Chemistry, Mashhad Branch, Islamic Azad University, Mashhad, I.R. IRAN

4 Department of Medicinal Chemistry, School of Pharmacy, Ardabil University of Medical Sciences, Ardabil, I.R. IRAN


A few 2-aryl-1H-phenanthro [9,10-d] imidazoles were synthesized and assessed for their cytotoxicity against MCF-7, HepG2, and AGS cell lines using MTT assay. Cellular assessments showed that phenanthroimidazoles were extremely potent cytotoxic agents (sub-nanomolar IC50s). Maximum effect was recorded for para-N-phenyl acetamide containing derivative against AGS cells (IC50 0.07 nM). It was also revealed that phenanthroimidazole derivatives showed better cytotoxicity against MCF-7 and AGS cells when compared to HepG2 cells. Minimum cytotoxicity was reported for para-methylphenyl derivatives within HepG2 cancer cells (IC50 7608.07 nM). Structure-activity relationship studies indicated that incorporation of nitrogen/oxygen-containing polar groups such as N-acetyl or nitro into para/meta positions of phenyl ring significantly enhanced the cytotoxicity against AGS cells. A similar trend was observed in meta-nitro derivatives vs MCF-7 cells. It was revealed that even the least potent compound exhibited cytotoxic activity in the range of low micromolar IC50. Results of this study proposed 2-aryl-1H-phenanthro [9,10-d] imidazoles as privileged structures for further in vivo studies.


Main Subjects

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