Design and synthesis of anti–inflammatory 1,2,3–triazolylpyrrolobenzodiazepinone derivatives and impact of molecular structure on COX–2 selective targeting
Journal of Molecular Structure(2023)
摘要
•Synthesis of a focused library of novel triazolylpyrrolobenzodaizepinone derivatives.•Compound (4l) showed extraordinary in vitro COX–2 inhibition (IC50 = 18.9 nM)].•It also showed the best selectivity (COX–1/COX–2 = 1060).•It acted as effective in vivo anti–inflammatory activity without inducing gastric ulceration.•Was found safe in cell toxicity studies on hela cells.•Compound (4l) could act as a potential lead candidate.
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关键词
Heterocyclic,Pyrrolobenzodiazepinone,COX–2,Anti–inflammatory,Triazoles,HeLa cells
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