Design and optimization of piperlongumine analogs as potent senolytics.
Bioorg Med Chem Lett
; 98: 129593, 2024 Jan 15.
Article
em En
| MEDLINE
| ID: mdl-38104906
ABSTRACT
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,ß-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.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Senescência Celular
/
Senoterapia
Idioma:
En
Ano de publicação:
2024
Tipo de documento:
Article