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Fluorophore-labeled cyclooxygenase-2 Inhibitors for the Imaging of cyclooxygenase-2 Overexpression in Cancer: Synthesis and Biological Studies

Fluorophore-labeled cyclooxygenase-2 Inhibitors for the Imaging of cyclooxygenase-2 Overexpression in Cancer: Synthesis and Biological Studies

Atul Bhardwaj, Jatinder Kaur, Frank Wuest, Edward E Knaus

ChemMedChem. 2014 Jan;9(1):109-16, 240.

PMID: 24376205

Abstract:

A group of cyclooxygenase-2 (COX-2)-specific fluorescent cancer biomarkers were synthesized by linking the anti-inflammatory drugs ibuprofen, (S)-naproxen, and celecoxib to the 7-nitrobenzofurazan (NBD) fluorophore. In vitro COX-1/COX-2 inhibition studies indicated that all of these fluorescent conjugates are COX-2 inhibitors (IC₅₀ range: 0.19-23.0 μM) with an appreciable COX-2 selectivity index (SI≥4.3-444). In this study the celecoxib-NBD conjugate N-(2-((7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)amino)ethyl)-4-(5-(p-tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, which displayed the highest COX-2 inhibitory potency and selectivity (COX-2 IC₅₀ =0.19 μM; SI=443.6), was identified as an impending COX-2-specific biomarker for the fluorescence imaging of cancer using a COX-2-expressing human colon cancer cell line (HCA-7).

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
IAR4242746	Celecoxib-NBD			Price

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