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

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 IC(50)s). 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. The results of this study proposed 2-aryl-1H-phenanthro [9,10-d] imidazoles as privileged structures for further in vivo studies.

Automated summary

In this study, several arylphenanthroimidazole derivatives were synthesized and evaluated for their cytotoxicity. The results showed that these compounds exhibited strong cytotoxic activity, with one derivative showing the highest effect against AGS cells. Structure-activity relationship studies indicated that incorporating nitrogen/oxygen-containing polar groups significantly enhanced cytotoxicity against AGS cells.