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

[Display omitted] 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 bisdemethoxycurcumi...

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Published in:Bioorganic & medicinal chemistry letters 2015-03, Vol.25 (5), p.1021-1025
Main Authors: Roman, Bart I., De Ryck, Tine, Verhasselt, Sigrid, Bracke, Marc E., Stevens, Christian V.
Format: Article
Language:English
Subjects:
Animals
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Cancer
Cell Line, Tumor
Chalcone
Chalcones - chemistry
Chalcones - pharmacology
Chickens
Curcumin - analogs & derivatives
Curcumin - pharmacology
Curcuminoids
Halogenation
Heart - drug effects
Humans
Invasion
Neoplasm Invasiveness - pathology
Neoplasm Invasiveness - prevention & control
Neoplasms - drug therapy
Neoplasms - pathology
SAR
Structure-Activity Relationship
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Summary:[Display omitted] 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2015.01.027