Ras, a GTP-binding protein involved in cell growth and oncogenesis, undergoes post-translational modification in three steps, the first of which is the farnesylation of a cysteine residue, mediated by farnesyltransferase (FTase). Therefore, FTase inhibitors (FTis) have potential therapeutic indications. Here, we report a series of analogues of FTi 1, obtained by replacement of o-tolyl with other aromatic residues (compounds 2-7) and, moreover, of (2-amino-4-thiazolyl)methyl with 1,4-benzodioxan-2-yl (compounds 8-13), as well as their isopropyl esters 2a-13a. The effect on protein farnesylation was tested using a Ftase fluorescent assay and FTI-276 as a reference compound.
|Titolo:||Design, synthesis and biological evaluation of peptidomimetic inhibitors of farnesyltransferase|
STRANIERO, VALENTINA (Primo)
|Data di pubblicazione:||22-set-2012|
|Settore Scientifico Disciplinare:||Settore CHIM/06 - Chimica Organica|
Settore CHIM/08 - Chimica Farmaceutica
|Citazione:||Design, synthesis and biological evaluation of peptidomimetic inhibitors of farnesyltransferase / V. Straniero, G. Chiodini, N. Ferri, M. Zagami, M. Pallavicini, E. Valoti. ((Intervento presentato al convegno IASOC tenutosi a Ischia nel 2012.|
|Appare nelle tipologie:||14 - Intervento a convegno non pubblicato|