Design and optimization of piperlongumine analogs as potent senolytics

Xuan Zhang, Yonghan He, Xingui Liu, Xin Zhang, Peizhong Shi, Yingying Wang, Daohong Zhou, Guangrong Zheng

Producción científica: Articlerevisión exhaustiva

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Selective removal of senescent cells (SnCs) offers a promising therapeutic strategy to treat chronic and age-related diseases. Our prior investigations led to the discovery of piperlongumine (PL) and its derivatives as senolytic agents. 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.

Idioma originalEnglish (US)
Número de artículo129593
PublicaciónBioorganic and Medicinal Chemistry Letters
EstadoPublished - ene 15 2024

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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