Chemistry

Biography

Biography: Gabriele Micheletti

Abstract

The research of compounds able to inhibit the interaction between APC/C and CDC20 has strongly emerged gaining a great deal of interest in recent years as useful tool for the design of CDC20 inhibitors, providing a therapeutic window in multiple human malignancies. Recently it has been discovered a new molecule called Apcin, which binds to CDC20, inhibiting the anaphase promoting complex into cells afflicted by AML (acute myeloid leukemia).  In this context we planned the synthesis of a series of Apcin analogues (Figure 1), characterized by an amino aza-heterocycle moiety (in blue), bounded to a trichloroethyl group (in green) in turn functionalized with a pletora of group (in red) inserted through nucleophilic substitution to the precursor. Preliminary biological tests were carried out on the compounds obtained towards a panel of solid and hematological cancer cell lines.