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4-Fluoro-3',4',5'-trimethoxychalcone as a new anti-invasive agent. From discovery to initial validation in an in vivo metastasis model.

Abstract：

:Invasion and metastasis are responsible for 90% of cancer-related mortality. Herein, we report on our quest for novel, clinically relevant inhibitors of local invasion, based on a broad screen of natural products in a phenotypic assay. Starting from micromolar chalcone hits, a predictive QSAR model for diaryl propenones was developed, and synthetic analogues with a 100-fold increase in potency were obtained. Two nanomolar hits underwent efficacy validation and eADMET profiling; one compound was shown to increase the survival time in an artificial metastasis model in nude mice. Although the molecular mechanism(s) by which these substances mediate efficacy remain(s) unrevealed, we were able to eliminate the major targets commonly associated with antineoplastic chalcones.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Roman BI,De Ryck T,Patronov A,Slavov SH,Vanhoecke BW,Katritzky AR,Bracke ME,Stevens CV

doi

10.1016/j.ejmech.2015.06.029

subject

Has Abstract

pub_date

2015-08-28 00:00:00

pages

627-39

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(15)30104-5

journal_volume

101

pub_type

杂志文章

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