📜吲哚美辛置于三甲基氯硅烷,Sodium Hydroxide体系中,用 水 作为反应溶剂,化学反应生成 5-甲氧基-2-甲基-3-吲哚乙酸甲酯
参考文献:Bifunctional Conjugates With Potent Inhibitory Activity Towards Cyclooxygenase And Histone Deacetylase
标题:Bifunctional Conjugates With Potent Inhibitory Activity Towards Cyclooxygenase And Histone Deacetylase
摘要:We Herein Disclose A Series Of Compounds With Potent Inhibitory Activities Towards Histone Deacetylases (Hdac) And Cyclooxygenases (Cox). These Compounds Potently Inhibited The Growth Of Cancer Cell Lines Consistent With Their Anti-Cox And Anti-Hdac Activities. While Compound 2B Showed Comparable Level Of Cox-2 Selectivity As Celecoxib,Compound Lib Outperformed Indomethacin In Terms Of Selectivity Towards Cox-2 Relative To Cox-1. An Important Observation With Our Lead Compounds (2B,8,11B,And 17B) Is Their Enhanced Cytotoxicity Towards Androgen Dependent Prostate Cancer Cell Line (Lncap) Relative To Androgen Independent Prostate Cancer Cell Line (Du-145). Interestingly,Compounds 2B And 17B Arrested The Cell Cycle Progression Of Lncap In The S-Phase,While Compound 8 Showed A G0/g1 Arrest,Similar To Saha. Relative To Saha,These Compounds Displayed Tumor-Selective Cytotoxicity As They Have Low Anti-Proliferative Activity Towards Healthy Cells (Vero); An Attribute That Makes Them Attractive Candidates For Drug Development. (C) 2016 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmc.2016.12.032