Title: Diketoacid chelating ligands as dual inhibitors of HIV-1 integration process
Authors: Rogolino, Dominga
Carcelli, Mauro
Compari, Carlotta
De Luca, Laura
Ferro, Stefania
Fisicaro, Emilia
Rispoli, Gabriele
Neamati, Nouri
Debyser, Zeger
Christ, Frauke
Chimirri, Alba # ×
Issue Date: May-2014
Series Title: European Journal of Medicinal Chemistry vol:78 pages:425-430
Article number: 10.1016/j.ejmech.2014.03.070
Abstract: HIV-1 Integrase (IN) represents a very attractive pharmacological target for the development of new and more efficient drugs. Recently, an allosteric inhibitory approach also emerged, that targets the interaction between IN and cellular cofactors, such as LEDGF/p75. Small molecules based on the diketoacid pharmachophore were studied for their ability to inhibit at the same time integration and IN-LEDGF/p75 interaction (dual inhibitors): in this study, we evaluated three indole diketoacid derivatives and their magnesium(II) complexes for their ability to act as dual inhibitors. Effectively, the metal complexes exhibited IN inhibition potency in low nanomolar/micromolar concentration range; both the complexes and the free ligands are also able to inhibit the IN-LEDGF/p75 interaction at low μM values. Moreover, these magnesium compounds showed good antiviral activity, suggesting the possibility to exploit metal coordination for the design of new antivirals.
ISSN: 0223-5234
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Molecular Virology and Gene Therapy
× corresponding author
# (joint) last author

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