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

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2,3-Diaryl-3-imidazo4,5-pyridine derivatives as potential anticancer and anti-inflammatory agents.

Author: Erin Marie KIRWEN ¹ ; Tarun BATRA ² ; Chandrabose KARTHIKEYAN ² ; Girdhar Singh DEORA ³ ; Vandana RATHORE ⁴ ; Chaitanya MULAKAYALA ⁵ ; Naveen MULAKAYALA ⁶ ; Amy Catherine NUSBAUM ¹ ; Joel CHEN ¹ ; Haneen AMAWI ¹ ; Kyle MCINTOSH ¹ ; Sahabjada ⁷ ; Neelam SHIVNATH ⁷ ; Deepak CHOWARSIA ² ; Nisha SHARMA ⁸ ; Md ARSHAD ⁷ ; Piyush TRIVEDI ² ; Amit K TIWARI ¹
Author Information

1. Department of Pharmacology and Experimental Therapeutics, College of Pharmacy & Pharmaceutical Sciences, University of Toledo, Toledo, OH 43614, USA.
2. School of Pharmaceutical Sciences, Rajiv Gandhi Technical University, Gandhi Nagar, Bhopal, MP 462036, India.
3. The University of Queensland, School of Pharmacy, Brisbane, Qld 4072, Australia.
4. The University of Queensland, School of Pharmacy, Brisbane, Qld 4072, Australia
5. Department of Biosciences, Sri Satya Sai Institute of Higher Learning, Anantapur campus, Andhra Pradesh 515001, India.
6. Clearsynth Labs Ltd., Research Centre, IDA-Mallapur, Hyderabad 500076, India.
7. Molecular Endocrinology Lab, Department of Zoology, University of Lucknow, Lucknow, UP 226007, India.
8. University Institute of Pharmacy, Chhatrapati Shahu Ji Maharaj University, Kanpur, UP 208024, India.
Publication Type:Journal Article
Keywords: 3H-Imidazo[4,5-b]pyri-dine; COX inhibitors; Cytotoxicity; Docking studies; MTT assay
From: Acta Pharmaceutica Sinica B 2017;7(1):73-79
CountryChina
Language:English
Abstract: 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.