Title:Synthesis and Physicochemical Characterization of Novel Phenotypic Probes Targeting the Nuclear Factor-kappa B Signaling Pathway

标题：新型表型探针的合成及理化性质表征：以核因子-κB信号通路为目标

Authors: Paul M. Hershberger, Satyamaheshwar Peddibhotla, E. Hampton Sessions, Daniela B. Divlianska, Ricardo G. Correa, Anthony B. Pinkerton, John C. Reed, Gregory P. Roth

Journal: Beilstein Journal of Organic Chemistry

Publication Date: May 8, 2013

Volume: 9

Pages: 900-907

DOI: 10.3762/bjoc.9.103

摘要
本研究报告了针对NF-κB信号通路的苯并咪唑和噁唑衍生物的新型化学探针的合成和物理化学特性表征。这些探针显示了显著的选择性和效力，为治疗涉及该通路的疾病提供了有希望的候选药物。

Abstract

This study reports the synthesis and physicochemical characterization of novel benzimidazole and oxazole derivatives as chemical probes targeting the NF-κB signaling pathway. These probes showed significant selectivity and potency, offering promising candidates for treating diseases involving this pathway.

背景
核因子κB（NF-κB）信号通路在炎症、免疫应答和细胞存活中起关键作用。抑制该通路的活性被认为对治疗多种疾病（如癌症和炎症性疾病）具有重要潜力。

Background

The nuclear factor-kappa B (NF-κB) signaling pathway plays a critical role in inflammation, immune responses, and cell survival. Inhibiting this pathway's activity is considered to have significant potential for treating various diseases, including cancer and inflammatory disorders.

方法
研究人员合成了一系列新的苯并咪唑和噁唑衍生物，并对其进行了物理化学特性表征和生物学评价。

Methods

The researchers synthesized a series of novel benzimidazole and oxazole derivatives and characterized their physicochemical properties and biological activities.

结果
研究发现了三种显著的探针：ML029、ML236和ML237，它们在生物化学和细胞模型中展示了对NF-κB的选择性抑制作用。

Results

The study identified three significant probes: ML029, ML236, and ML237, which demonstrated selective inhibition of NF-κB in biochemical and cellular models.

结论
该研究成功开发了几种针对NF-κB信号通路的高效选择性探针，这些探针有望用于治疗涉及该通路的疾病。

Conclusion

The study successfully developed several potent and selective probes targeting the NF-κB signaling pathway, which hold promise for treating diseases involving this pathway.