Synthesis and in vivo modulatory activity of protein kinase C of xanthone derivatives

• Type: Article in International Scientific Journal
• Date: 2002

Authors

Saraiva, L (Author) FFUP; Fresco, P (Author) FFUP; Pinto, E (Author) FFUP; Sousa, E (Author) Other; Pinto, M (Author) FFUP; Goncalves, J (Author) FFUP

Journal

Title: Bioorganic and Medicinal Chemistry

Vol. 10

Pages: 3219-3227

ISSN: 0968-0896

Publisher: Elsevier

Indexing

ISI Proceedings

ISI Web of Knowledge - 42 Citations

Scopus - 44 Citations

Scientific classification

FOS: Natural sciences > Chemical sciences

Other information

Authenticus ID: P-000-MRY

DOI: 10.1016/s0968-0896(02)00169-4

Abstract (EN): 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.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 9