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Further studies on anti-invasive chemotypes: An excursion from chalcones to curcuminoids.

Abstract：

:In our ongoing search for new anti-invasive chemotypes, we have made an excursion from previously reported potent 1,3-diarylpropenones (chalcones) to congeners bearing longer linkers between the aromatic moieties. Nine 1,ω-diarylalkenones, including curcumin and bisdemethoxycurcumin, were evaluated in the chick heart invasion assay. Unfortunately, these compounds proved less potent and more toxic than earlier evaluated chemotypes. In the 1,3-diarylpenta-2,4-dien-1-one series, fluoro and/or trimethoxy substitution caused an increase in potency. This agrees with observations made earlier for the chalcone class.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Roman BI,De Ryck T,Verhasselt S,Bracke ME,Stevens CV

doi

10.1016/j.bmcl.2015.01.027

subject

Has Abstract

pub_date

2015-03-01 00:00:00

pages

1021-5

issue

5

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(15)00039-6

journal_volume

25

pub_type

杂志文章

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