Synthesis, characterization, and antileishmanial activities of gold(I) complexes involving quinoline functionalized N-heterocyclic carbenes

European Journal of Medicinal Chemistry
Lucie PaloqueHeinz Gornitzka

Abstract

A series of new mononuclear cationic or neutral gold(I) complexes containing quinoline functionalized N-heterocyclic carbene(s) (NHC(s)) were synthesized and fully characterized by spectroscopic methods. The X-ray structures of two key compounds are presented. Proligands and their corresponding gold(I) complexes together with previously described silver(I) and gold(I) bis(NHC-quinoline) and gold(I) bis(NHC-methylbipyridine) complexes were evaluated in vitro towards Leishmania infantum. In parallel, the in vitro cytotoxicity of these molecules was assessed on the murine macrophages J774A.1. All gold(I) compounds show potent antileishmanial activity against L. infantum promastigotes and three of them are also efficient against L. infantum intracellular amastigotes. Structure-activity and toxicity relationships enables to evidence a lead-compound (6) displaying both a high activity and a good selectivity index.

References

Mar 9, 2013·Mini Reviews in Medicinal Chemistry·Kristie A ReynoldsDavid J Young
Nov 21, 2014·Expert Opinion on Investigational Drugs·Shyam Sundar, Jaya Chakravarty

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Citations

Nov 9, 2016·European Journal of Medicinal Chemistry·Joana Darc S ChavesMauro V de Almeida
Dec 4, 2015·Dalton Transactions : an International Journal of Inorganic Chemistry·Catherine Hemmert, Heinz Gornitzka
Dec 7, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Xiu E FengQing Shan Li
Sep 14, 2018·Journal of Biological Inorganic Chemistry : JBIC : a Publication of the Society of Biological Inorganic Chemistry·G Y Sánchez DelgadoH F Dos Santos
Nov 27, 2018·Chemical Society Reviews·Malka MoraRenso Visbal
Apr 28, 2019·Molecular Diversity·Nima Razzaghi-AslMohammad Johari-Ahar
Jan 31, 2016·Anti-cancer Drugs·Rakibe B BostancioğluKadriye Benkli
Jun 24, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Manel OujiHeinz Gornitzka
Dec 7, 2018·Chemical Reviews·Yih Ching OngGilles Gasser

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