Discovery of 5-sulfonyltetrazoles as neuroblastoma differentiation agents.
Bioorg Med Chem Lett
; 94: 129455, 2023 10 01.
Article
em En
| MEDLINE
| ID: mdl-37597697
ABSTRACT
Previously, we developed an innovative high-content screening (HCS) approach to quantify neuroblastoma cell differentiation based on neurite outgrowth, a morphological differentiation marker of neuroblastoma cells. Here, we report the utilization of this platform to identify 1-methyl-5-(ethylsulfonyl)-1H-tetrazole (3a) as a new neuroblastoma differentiation agent using the ChemBridge DiversetTM commercial synthetic small molecule compound library. We show that this activity can be extended to a group of analogues, which can be accessed via a short two-step synthetic sequence. A new analogue, 5-(allylsulfonyl)-1-methyl-1H-tetrazole (3c) was identified in this synthetic effort as a compound that has even more pronounced differentiation and cytotoxic activities than the original hit compound 3a.
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Texto completo:
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Neuroblastoma
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2023
Tipo de documento:
Article