2,3-Diaryl-3H-imidazo[4,5-b]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

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In this study we examined the suitability of the 3H-imidazo[4,5-b]pyridine ring system in developing novel anticancer and anti-inflammatory agents incorporating a diaryl pharmacophore. Eight 2,3-diaryl-3H-imidazo[4,5-b]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-3H-imidazo[4,5-b]pyridine derivatives were also evaluated for their COX-1 and COX-2 inhibitory activity in vitro. The results showed that compound 3f exhibited 2-fold selectivity with IC50 values of 9.2 and 21.8 µmol/L against COX-2 and COX-1, respectively. Molecular docking studies on the most active compound 3f revealed a binding mode similar to that of celecoxib in the active site of the COX-2 enzyme.

Original languageEnglish
Pages (from-to)73-79
Number of pages7
JournalActa Pharmaceutica Sinica B
Issue number1
Publication statusPublished - 1 Jan 2017
Externally publishedYes


  • 3H-Imidazo[4,5-b]pyri-dine
  • COX inhibitors
  • Cytotoxicity
  • Docking studies
  • MTT assay

Cite this

Marie Kirwen, E., Batra, T., Karthikeyan, C., Deora, G. S., Rathore, V., Mulakayala, C., Mulakayala, N., Nusbaum, A. C., Chen, J., Amawi, H., McIntosh, K., Sahabjada, Shivnath, N., Chowarsia, D., Sharma, N., Arshad, M., Trivedi, P., & Tiwari, A. K. (2017). 2,3-Diaryl-3H-imidazo[4,5-b]pyridine derivatives as potential anticancer and anti-inflammatory agents. Acta Pharmaceutica Sinica B, 7(1), 73-79. https://doi.org/10.1016/j.apsb.2016.05.003