1.2,3-Diaryl-3-imidazo4,5-pyridine derivatives as potential anticancer and anti-inflammatory agents.
Erin Marie KIRWEN ; Tarun BATRA ; Chandrabose KARTHIKEYAN ; Girdhar Singh DEORA ; Vandana RATHORE ; ; Chaitanya MULAKAYALA ; Naveen MULAKAYALA ; Amy Catherine NUSBAUM ; Joel CHEN ; Haneen AMAWI ; Kyle MCINTOSH ; Sahabjada ; Neelam SHIVNATH ; Deepak CHOWARSIA ; Nisha SHARMA ; Md ARSHAD ; Piyush TRIVEDI ; Amit K TIWARI
Acta Pharmaceutica Sinica B 2017;7(1):73-79
In this study we examined the suitability of the-imidazo[4,5-]pyridine ring system in developing novel anticancer and anti-inflammatory agents incorporating a diaryl pharmacophore. Eight 2,3-diaryl-3-imidazo[4,5-]pyridine derivatives retrieved from our in-house database were evaluated for their cytotoxic activity against nine cancer cell lines. The results indicated that the compounds showed moderate cytotoxic activity against MCF-7, MDA-MB-468, K562 and SaOS2 cells, with K562 being the most sensitive among the four cancer cell lines. The eight 2,3-diaryl-3-imidazo[4,5-]pyridine derivatives were also evaluated for their COX-1 and COX-2 inhibitory activity. The results showed that compoundexhibited 2-fold selectivity with ICvalues of 9.2 and 21.8 µmol/L against COX-2 and COX-1, respectively. Molecular docking studies on the most active compoundrevealed a binding mode similar to that of celecoxib in the active site of the COX-2 enzyme.
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