Publications des scientifiques de l'IRD

Ftouh S., Bourgeade-Delmas Sandra, Belkadi M., Deraeve C., Hemmert C., Valentin A., Gornitzka H. (2021). Synthesis, characterization, and antileishmanial activity of neutral gold(I) complexes with N-heterocyclic carbene ligands bearing sulfur-containing side arms. Organometallics, 40 (10), p. 1466-1473. ISSN 0276-7333.

Titre du document
Synthesis, characterization, and antileishmanial activity of neutral gold(I) complexes with N-heterocyclic carbene ligands bearing sulfur-containing side arms
Année de publication
2021
Type de document
Article référencé dans le Web of Science WOS:000656119500006
Auteurs
Ftouh S., Bourgeade-Delmas Sandra, Belkadi M., Deraeve C., Hemmert C., Valentin A., Gornitzka H.
Source
Organometallics, 2021, 40 (10), p. 1466-1473 ISSN 0276-7333
With an estimated annual incidence of one million cases, leishmaniasis is one of the top five vector-borne diseases. Currently available medical treatments involve side effects, including toxicity, nonspecific targeting, and resistance development. Thus, new antileishmanial chemical entities are of the utmost importance to fight against this disease. We have shown in previous studies that gold(I) complexes bearing N-heterocyclic carbene (NHC) ligands with nitrogen- or sulfur-containing side arms have interesting biological activities in the field of cancer, malaria and leishmaniasis. The present study evaluates the in vitro antileishmanial effects on L. infantum axenic amastigotes and their cytotoxicity for the human THP1 cell line of a new family of six new imidazolium salts and their corresponding neutral (NHC)(AuCl)-Cl-I complexes. All new compounds have been characterized by classical analytical methods, and five gold complexes have been analyzed by X-ray structure determinations. We showed that one proligand has moderate activity (IC50 = 8.24 mu M) while four of the six gold complexes have IC50 values in the low or sub mu M range (0.15-1.3 mu M), including three with selectivity index (SI) values between 46 and 108. These results suggest remarkable leishmanicidal activity in vitro for three new neutral (NHC)Au(I)Cl complexes, making them candidates for further in vivo studies, which are under investigation.
Plan de classement
Sciences fondamentales / Techniques d'analyse et de recherche [020] ; Santé : généralités [050]
Localisation
Fonds IRD [F B010082082]
Identifiant IRD
fdi:010082082
Contact