Synthesis, characterization, and antileishmanial activity of neutral N-heterocyclic carbenes gold(I) complexes.

Authors :: Zhang C
Bourgeade Delmas S
Fernández Álvarez Á
Valentin A
Hemmert C
Gornitzka H
Source :: European journal of medicinal chemistry [Eur J Med Chem] 2018 Jan 01; Vol. 143, pp. 1635-1643. Date of Electronic Publication: 2017 Oct 24.
Publication Year :: 2018
Abstract: A series of five new mononuclear neutral gold(I) complexes containing N-heterocyclic carbenes (NHCs) was synthesized and fully characterized by spectroscopic methods. The X-ray structures of four complexes are presented. These gold(I) complexes together with four other neutral gold(I)-NHC complexes previously described were evaluated in vitro against Leishmania infantum promastigotes and axenic amastigotes. Moreover, their cytotoxicity was assessed on the murine macrophages J774A.1. Except one complex (10), eight gold(I)-NHC-Cl complexes show potent activity against the pathological relevant form of L. infantum amastigote with IC <subscript>50</subscript> in the low micromolar and submicromolar range and five of them exhibit a SI close to 10. The lead-complex 11 displays a very high and selective activity (IC <subscript>50</subscript>  = 190 nM, SI = 40.29) and constitutes the best promising gold(I)-based drug of this series.<br /> (Copyright © 2017 Elsevier Masson SAS. All rights reserved.)

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