title: 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.
authors: Research Group SynBioC, Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Coupure Links 653, B-9000 Ghent, Belgium. Electronic address: Bart1.Roman@UGent.be.
authors: Bart I
authors: BI
authors: Roman
authors: Laboratory of Experimental Cancer Research, Department of Radiation Oncology and Experimental Cancer Research, Ghent University, De Pintelaan 185, B-9000 Ghent, Belgium. Electronic address: Tine.DeRyck@UGent.be.
authors: Tine
authors: T
authors: De Ryck
authors: Research Group SynBioC, Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Coupure Links 653, B-9000 Ghent, Belgium.
authors: Sigrid
authors: S
authors: Verhasselt
authors: Laboratory of Experimental Cancer Research, Department of Radiation Oncology and Experimental Cancer Research, Ghent University, De Pintelaan 185, B-9000 Ghent, Belgium. Electronic address: Marc1.Bracke@UGent.be.
authors: Marc E
authors: ME
authors: Bracke
authors: Research Group SynBioC, Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Coupure Links 653, B-9000 Ghent, Belgium. Electronic address: Chris.Stevens@UGent.be.
authors: Christian V
authors: CV
authors: Stevens
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D047188:Chalcones / Q000737:chemistry* / Q000494:pharmacology; D002645:Chickens; D003474:Curcumin / Q000031:analogs & derivatives* / Q000494:pharmacology; D054879:Halogenation; D006321:Heart / Q000187:drug effects; D006801:Humans; D009361:Neoplasm Invasiveness / Q000473:pathology / Q000517:prevention & control*; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D047188:Chalcones; D003474:Curcumin
keywords: Cancer; Chalcone; Curcuminoids; Invasion; SAR