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Targeting gliomas with triazene-based hybrids: Structure-activity relationship, mechanistic study and stability.

Abstract：

: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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Braga C,Vaz AR,Oliveira MC,Matilde Marques M,Moreira R,Brites D,Perry MJ

doi

10.1016/j.ejmech.2019.03.048

subject

Has Abstract

pub_date

2019-06-15 00:00:00

pages

16-25

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(19)30271-5

journal_volume

172

pub_type

杂志文章

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