Anno2012
AutoriBianchi A; Ugazzi M; Ferrante L; Lecis D; Scavullo C; Mastrangelo E; Seneci P
AbstractA set of phenyl-substituted Smac mimetics/IAP inhibitor analogues of lead compound 2a was synthesized, aiming to retain its strong cell-free potency while increasing its bioavailability. Seventeen compounds 2b-r were prepared and characterized in vitro, using cell-free and cellular assays. Among them, the p-CF3 substituted analogue 2m showed the best permeability through cell membranes, and was selected for further in vitro and in vivo studies due to its strong, sub-micromolar cellular potency.
RivistaBioorganic & Medicinal Chemistry Letters
ISSN0960-894X
Impact factor
Volume22
Pagina inizio2208
Pagina fine2204
Autori IBFEloise MASTRANGELO
Linee di Ricerca IBFMD.P01.005.001
Sedi IBFIBF.MI