当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis and biological evaluation in U87MG glioma cells of (ethynylthiophene)sulfonamido-based hydroxamates as matrix metalloproteinase inhibitors.

Synthesis and biological evaluation in U87MG glioma cells of (ethynylthiophene)sulfonamido-based hydroxamates as matrix metalloproteinase inhibitors.

Abstract：

:Matrix metalloproteinases (MMPs) are important factors in gliomas since these enzymes facilitate invasion into the surrounding brain and participate in neovascularization. In particular, the gelatinases (MMP-2 and MMP-9), and more recently MMP-25, have been shown to be highly expressed in gliomas and have been associated with disease progression. Thus, inhibition of these MMPs may represent a promising non-cytotoxic approach to glioma treatment. We report herein the synthesis and biological evaluation of a series of 4-butylphenyl(ethynylthiophene)sulfonamido-based hydroxamates. Among the new compounds tested, a promising derivative, 5a, was identified, which exhibits nanomolar inhibition of MMP-2, MMP-9, and MMP-25, but weak inhibitory activity toward other members of the MMP family. This compound also exhibited anti-invasive activity of U87MG glioblastoma cells at nanomolar concentrations, without affecting cell viability.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Nuti E,Casalini F,Santamaria S,Gabelloni P,Bendinelli S,Da Pozzo E,Costa B,Marinelli L,La Pietra V,Novellino E,Margarida Bernardo M,Fridman R,Da Settimo F,Martini C,Rossello A

doi

10.1016/j.ejmech.2011.03.033

subject

Has Abstract

pub_date

2011-07-01 00:00:00

pages

2617-29

issue

7

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(11)00248-0

journal_volume

46

pub_type

杂志文章

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