title: Design, synthesis and structure-activity relationships of some novel, highly potent anti-invasive (E)- and (Z)-stilbenes.
abstract: In our ongoing exploration of the structure-activity landscape of anti-invasive chalcones, we have prepared and evaluated a number of structurally related (E)- and (Z)-stilbenes. These molecules exhibited an extraordinary high in vitro potency in the chick heart invasion assay, being active up to 10nmolL(-1), a concentration level a 100-fold lower than the lowest effective doses that have been reported for natural analogues. Furthermore, they possess an interesting pharmacological profile in silico.
authors.affiliation: Research Group SynBioC, Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Coupure Links 653, B-9000 Ghent, Belgium.
authors.forename: Bart I
authors.initials: BI
authors.lastname: Roman
authors.forename: Laurens M
authors.initials: LM
authors.lastname: De Coen
authors.forename: Séverine
authors.initials: S
authors.lastname: Thérèse F C Mortier
authors.forename: Tine
authors.initials: T
authors.lastname: De Ryck
authors.forename: Barbara W A
authors.initials: BW
authors.lastname: Vanhoecke
authors.forename: Alan R
authors.initials: AR
authors.lastname: Katritzky
authors.forename: Marc E
authors.initials: ME
authors.lastname: Bracke
authors.forename: Christian V
authors.initials: CV
authors.lastname: Stevens
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002465:Cell Movement / Q000187:drug effects; D047188:Chalcones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002645:Chickens; D015195:Drug Design; D005260:Female; D006321:Heart / Q000187:drug effects; D006801:Humans; D061986:MCF-7 Cells; D009924:Organ Culture Techniques; D013237:Stereoisomerism; D013267:Stilbenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D047188:Chalcones; D013267:Stilbenes
keywords: Cancer; Chalcone; Invasion; SAR; Stilbene