Design and Optimization of Piperlongumine Analogs as Potent Senolytics

In this study, our medicinal chemistry campaign on both the α,β-unsaturated δ-valerolactam ring and the phenyl ring of PL culminated in the identification of compound 24, which exhibited an impressive 50-fold enhancement in senolytic activity against senescent WI-38 fibroblasts compared to PL.PMID:38104906 | DOI:10.1016/j.bmcl.2023.129593

Source: Bioorganic and Medicinal Chemistry Letters - December 17, 2023 Category: Chemistry Authors: Xuan Zhang Yonghan He Xingui Liu Xin Zhang Peizhong Shi Yingying Wang Daohong Zhou Guangrong Zheng Source Type: research