Design, synthesis and biological evaluation of pyridine acyl sulfonamide derivatives as novel COX-2 inhibitors
2011
Lu, Xiang | Zhang, Hui | Li, Xi | Chen, Guo | Li, Qing-Shan | Luo, Yin | Ruan, Ban-Feng | Chen, Xian-Wei | Zhu, Hai-Liang
A series of pyridine acyl sulfonamide derivatives (1–24) have been designed and synthesized and their biological activities were also evaluated as potential cyclooxygenase-2 (COX-2) inhibitors. Among all the compounds, compound 23 displayed the most potent COX-2 inhibitory activity with an IC₅₀ of 0.8μM. Antitumor and anti-inflammatory assays indicated that compound 23 owned high antiproliferative activity against B16-F10, HepG2 and MCF-7 cancer cell lines as well as COX-2-derived prostaglandin E₂ (PGE₂) inhibitory activity of murine macrophage RAW 264.7 cell line with IC₅₀ values of 2.8, 1.2, 1.8 and 0.15μM, respectively. Docking simulation was performed to position compound 23 into the COX-2 active site to determine the probable binding model.
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Эту запись предоставил National Agricultural Library