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Optimization of troglitazone derivatives as potent anti-proliferative agents: towards more active and less toxic compounds.

Abstract：

:Δ2-Troglitazone derivatives were shown to exhibit anti-proliferative activity in a PPARγ-independent manner. We prepared various compounds in order to increase their potency and decrease their toxicity towards non-malignant primary cultured hepatocytes. Many compounds induced viabilities less than 20% at 10 μM on various cancer cell lines. Furthermore, five of them showed hepatocyte viability of 80% or more at 200 μM. In addition, compounds 17 and 18 exhibited promising maximum tolerated doses on a murine model, enabling future investigations.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Bordessa A,Colin-Cassin C,Grillier-Vuissoz I,Kuntz S,Mazerbourg S,Husson G,Vo M,Flament S,Martin H,Chapleur Y,Boisbrun M

doi

10.1016/j.ejmech.2014.06.015

subject

Has Abstract

pub_date

2014-08-18 00:00:00

pages

129-40

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(14)00534-0

journal_volume

83

pub_type

杂志文章

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