荧光标记的环氧化酶-2 抑制剂用于癌症中环氧化酶-2 过表达的成像：合成与生物学研究。
Fluorophore-labeled cyclooxygenase-2 inhibitors for the imaging of cyclooxygenase-2 overexpression in cancer: synthesis and biological studies.
机构信息
Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Alberta, T6G 2E1 (Canada); Department of Oncology, Cross Cancer Institute, University of Alberta, Edmonton, Alberta, T6G 1Z2 (Canada).
出版信息
ChemMedChem. 2014 Jan;9(1):109-16, 240. doi: 10.1002/cmdc.201300355. Epub 2013 Oct 31.
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).
一组环氧化酶-2（COX-2）特异性荧光癌症生物标志物通过将抗炎药物布洛芬、（S）-萘普生和塞来昔布连接到 7-硝基苯并呋咱（NBD）荧光团上合成。体外 COX-1/COX-2 抑制研究表明，所有这些荧光缀合物都是 COX-2 抑制剂（IC₅₀范围：0.19-23.0 μM），具有可观的 COX-2 选择性指数（SI≥4.3-444）。在这项研究中，塞来昔布-NBD 缀合物 N-(2-((7-硝基苯并[c][1,2,5]恶二唑-4-基)氨基)乙基)-4-(5-(对甲苯基)-3-(三氟甲基)-1H-吡唑-1-基)苯磺酰胺，显示出最高的 COX-2 抑制效力和选择性（COX-2 IC₅₀=0.19 μM；SI=443.6），被鉴定为使用表达 COX-2 的人结肠癌细胞系（HCA-7）进行癌症荧光成像的潜在 COX-2 特异性生物标志物。
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