Semisynthetic derivatives of parthenolide (1) were tested on NF-kB driven transcription and metalloproteinase- 9 (MMP-9) expression and secretion. The four membered ring compounds 5 and 6, obtained by acidic treatment of 1, exhibited a higher activity with respect to 1 in all the biological assays. Then an increased ability of the 5 and 6 to inhibit NF-kB driven transcription may lead to a down-regulation of MMP-9 expression and secretion. This work provides new details about the structural requisites for NF-kB inhibition
Inhibition of NF-kB and metalloproteinase-9 expression and secretion by parthenolide derivatives / M. Dell'Agli, G. Galli, E.A. Bosisio, M. D'Ambrosio. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 19:7(2009), pp. 1858-1860.
Inhibition of NF-kB and metalloproteinase-9 expression and secretion by parthenolide derivatives
M. Dell'AgliPrimo
;G. GalliSecondo
;E.A. BosisioPenultimo
;
2009
Abstract
Semisynthetic derivatives of parthenolide (1) were tested on NF-kB driven transcription and metalloproteinase- 9 (MMP-9) expression and secretion. The four membered ring compounds 5 and 6, obtained by acidic treatment of 1, exhibited a higher activity with respect to 1 in all the biological assays. Then an increased ability of the 5 and 6 to inhibit NF-kB driven transcription may lead to a down-regulation of MMP-9 expression and secretion. This work provides new details about the structural requisites for NF-kB inhibition
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