期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 172, 期 -, 页码 16-25出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.03.048
关键词
Triazenes; Histone deacetylase inhibitors; Valproic acid; Multi-targeted glioma therapy
资金
- Fundacao para a Ciencia e Tecnologia (FCT, Portugal) [UID/00100/2013, UID/04138/2013]
- FCT [PD/BD/128239/2016, SAICTPAC/0019/2015]
- COMPETE Program [SAICTPAC/0019/2015]
- Portugal 2020 [RNEM LISBOA-01-0145-FEDER-402-022125 IST]
- Fundação para a Ciência e a Tecnologia [PD/BD/128239/2016] Funding Source: FCT
Herein we report novel hybrid compounds based on valproic acid and DNA-alkylating triazene moieties, 1, with therapeutic potential for glioblastoma multiforme chemotherapy. We identified hybrid compounds 1d and 1e to be remarkably more potent against glioma and more efficient in decreasing invasive cell properties than temozolomide and endowed with chemical and plasma stability. In contrast to temozolomide, which undergoes hydrolysis to release an alkylating metabolite, the valproate hybrids showed a low potential to alkylate DNA. Key physicochemical properties align for optimal CNS penetration, highlighting the potential of these effective triazene based-hybrids for enhanced anticancer chemotherapy. (C) 2019 Elsevier Masson SAS. All rights reserved.
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