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Synthesis and biological evaluation of novel apcin analogues as potential CDC20 inhibitors


14th World Congress on Chemistry

April 03-04, 2023 | Barcelona, Spain

Gabriele Micheletti*, Carla Boga, Natalia Calonghi and Giorgia Simonetti

University of Bologna, Italy

ScientificTracks Abstracts: JCHEM

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.

Biography

Gabriele Micheletti is currently in the Department of Industrial Chemistry at the University of Bologna. His field of specialization is organic chemistry and he has completed his studies in Industrial Chemistry in 2006, at the Faculty of Industrial Chemistry University of Bologna, Italy. In the 2011 he has pursued his PhD in Chemical Sciences at the same University. His fields of expertise are synthesis of novel organic compounds, organophosphorus chemistry, studies on mechanisms of organic chemistry reactions especially through detection of labile reaction intermediates by NMR spectroscopy (heteronuclear, dynamic variable temperature). Recent interest is in synthesis of new organic compounds of possible interest in biological field. He has more than 60 research publications in peer reviewed international journals.