title: 2,3-Diaryl-3H-imidazo[4,5-b]pyridine derivatives as potential anticancer and anti-inflammatory agents.
abstract: In this study we examined the suitability of the3H-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 activityin vitro. The results showed that compound3fexhibited 2-fold selectivity with IC50values of 9.2 and 21.8 µmol/L against COX-2 and COX-1, respectively. Molecular docking studies on the most active compound3frevealed a binding mode similar to that of celecoxib in the active site of the COX-2 enzyme.
authors.affiliation: Department of Pharmacology and Experimental Therapeutics, College of Pharmacy & Pharmaceutical Sciences, University of Toledo, Toledo, OH 43614, USA.
authors.forename: Erin
authors.initials: E
authors.lastname: Marie Kirwen
authors.affiliation: School of Pharmaceutical Sciences, Rajiv Gandhi Technical University, Gandhi Nagar, Bhopal, MP 462036, India.
authors.forename: Tarun
authors.initials: T
authors.lastname: Batra
authors.affiliation: School of Pharmaceutical Sciences, Rajiv Gandhi Technical University, Gandhi Nagar, Bhopal, MP 462036, India.
authors.forename: Chandrabose
authors.initials: C
authors.lastname: Karthikeyan
authors.affiliation: The University of Queensland, School of Pharmacy, Brisbane, Qld 4072, Australia.
authors.forename: Girdhar Singh
authors.initials: GS
authors.lastname: Deora
authors.affiliation: The University of Queensland, School of Pharmacy, Brisbane, Qld 4072, Australia; Dr. Reddy׳s Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India; The University of Queensland, School of Biomedical Sciences, Brisbane, Qld 4072, Australia.
authors.forename: Vandana
authors.initials: V
authors.lastname: Rathore
authors.affiliation: Department of Biosciences, Sri Satya Sai Institute of Higher Learning, Anantapur campus, Andhra Pradesh 515001, India.
authors.forename: Chaitanya
authors.initials: C
authors.lastname: Mulakayala
authors.affiliation: Clearsynth Labs Ltd., Research Centre, IDA-Mallapur, Hyderabad 500076, India.
authors.forename: Naveen
authors.initials: N
authors.lastname: Mulakayala
authors.affiliation: Department of Pharmacology and Experimental Therapeutics, College of Pharmacy & Pharmaceutical Sciences, University of Toledo, Toledo, OH 43614, USA.
authors.forename: Amy Catherine
authors.initials: AC
authors.lastname: Nusbaum
authors.affiliation: Department of Pharmacology and Experimental Therapeutics, College of Pharmacy & Pharmaceutical Sciences, University of Toledo, Toledo, OH 43614, USA.
authors.forename: Joel
authors.initials: J
authors.lastname: Chen
authors.affiliation: Department of Pharmacology and Experimental Therapeutics, College of Pharmacy & Pharmaceutical Sciences, University of Toledo, Toledo, OH 43614, USA.
authors.forename: Haneen
authors.initials: H
authors.lastname: Amawi
authors.affiliation: Department of Pharmacology and Experimental Therapeutics, College of Pharmacy & Pharmaceutical Sciences, University of Toledo, Toledo, OH 43614, USA.
authors.forename: Kyle
authors.initials: K
authors.lastname: McIntosh
authors.affiliation: Molecular Endocrinology Lab, Department of Zoology, University of Lucknow, Lucknow, UP 226007, India.
authors.lastname: Sahabjada
authors.affiliation: Molecular Endocrinology Lab, Department of Zoology, University of Lucknow, Lucknow, UP 226007, India.
authors.forename: Neelam
authors.initials: N
authors.lastname: Shivnath
authors.affiliation: School of Pharmaceutical Sciences, Rajiv Gandhi Technical University, Gandhi Nagar, Bhopal, MP 462036, India.
authors.forename: Deepak
authors.initials: D
authors.lastname: Chowarsia
authors.affiliation: University Institute of Pharmacy, Chhatrapati Shahu Ji Maharaj University, Kanpur, UP 208024, India.
authors.forename: Nisha
authors.initials: N
authors.lastname: Sharma
authors.affiliation: Molecular Endocrinology Lab, Department of Zoology, University of Lucknow, Lucknow, UP 226007, India.
authors.forename: Md
authors.initials: M
authors.lastname: Arshad
authors.affiliation: School of Pharmaceutical Sciences, Rajiv Gandhi Technical University, Gandhi Nagar, Bhopal, MP 462036, India.
authors.forename: Piyush
authors.initials: P
authors.lastname: Trivedi
authors.affiliation: Department of Pharmacology and Experimental Therapeutics, College of Pharmacy & Pharmaceutical Sciences, University of Toledo, Toledo, OH 43614, USA.
authors.forename: Amit K
authors.initials: AK
authors.lastname: Tiwari
keywords: 3H-Imidazo[4,5-b]pyri-dine; COX inhibitors; Cytotoxicity; Docking studies; MTT assay