Selective COX-2 inhibitors. Part 1: Synthesis and biological evaluation of phenylazobenzenesulfonamides

Wei Jern Tsai, Young Ji Shiao, Shwu Jiuan Lin, Wen Fei Chiou, Lie Chwen Lin, Tsang Hsiung Yang, Che Ming Teng, Tain Shung Wu, Li Ming Yang

研究成果: 雜誌貢獻文章

43 引文 斯高帕斯(Scopus)

摘要

A series of phenylazobenzenesulfonamide derivatives were designed and synthesized for the evaluation as selective cyclooxygenase-2 (COX-2) inhibitors in a cellular assay using human whole blood (HWB) and an enzymatic assay using purified ovine enzymes. Extensive structure-activity relationships (SAR) were studied within this series, and several of selective COX-2 inhibitors have been identified. Among them, compound 8, 4-(4-amino-2-methylsulfanyl-phenylazo)benzenesulfonamide, showed a potent inhibitory activity to the cyclooxygenase enzymes (IC50's for COX-1: 23.28 μM; COX-2: 2.04 μM), being active but less COX-2 selective than celecoxib.
原文英語
頁(從 - 到)4440-4443
頁數4
期刊Bioorganic and Medicinal Chemistry Letters
16
發行號17
DOIs
出版狀態已發佈 - 九月 1 2006

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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    Tsai, W. J., Shiao, Y. J., Lin, S. J., Chiou, W. F., Lin, L. C., Yang, T. H., Teng, C. M., Wu, T. S., & Yang, L. M. (2006). Selective COX-2 inhibitors. Part 1: Synthesis and biological evaluation of phenylazobenzenesulfonamides. Bioorganic and Medicinal Chemistry Letters, 16(17), 4440-4443. https://doi.org/10.1016/j.bmcl.2006.06.036