title: Synthesis and in vivo modulatory activity of protein kinase C of xanthone derivatives.
abstract: The modulatory activity of a series of 20 simple xanthones on isoforms alpha, betaI, delta, eta and zeta of protein kinase C (PKC) was evaluated using an in vivo yeast phenotypic assay. Hydroxy and/or methoxyxanthones were synthesised. The majority of these compounds caused an effect compatible with activation of PKC and some showed to be more effective than the standard PKC activator (PMA or arachidonic acid). The xanthones tested differ in their efficacy and potency towards individual PKC isoforms and some showed higher selectivities for PKC-delta, -eta or -zeta, suggesting that xanthone derivatives can become valuable research tools to elucidate the physiological roles of these isoforms.
authors.affiliation: Serviço de Farmacologia, Faculdade de Farmácia, Universidade do Porto, rua Aníbal Cunha, 164, Porto, Portugal.
authors.forename: Lucília
authors.initials: L
authors.lastname: Saraiva
authors.forename: Paula
authors.initials: P
authors.lastname: Fresco
authors.forename: Eugénia
authors.initials: E
authors.lastname: Pinto
authors.forename: Emília
authors.initials: E
authors.lastname: Sousa
authors.forename: Madalena
authors.initials: M
authors.lastname: Pinto
authors.forename: Jorge
authors.initials: J
authors.lastname: Gonçalves
mesh_terms: D000818:Animals; D002455:Cell Division / Q000187:drug effects; D004789:Enzyme Activation / Q000187:drug effects; D006801:Humans; D007527:Isoenzymes / Q000187:drug effects / Q000235:genetics; D008322:Mammals; D011493:Protein Kinase C / Q000187:drug effects* / Q000235:genetics; D013329:Structure-Activity Relationship; D014170:Transformation, Genetic; D014966:Xanthenes / Q000138:chemical synthesis* / Q000494:pharmacology; D044004:Xanthones; D015003:Yeasts / Q000166:cytology / Q000235:genetics
chemical_list: D007527:Isoenzymes; D014966:Xanthenes; D044004:Xanthones; C009689:xanthone; D011493:Protein Kinase C