Improved antiparasitic activity by incorporation of organosilane entities into half-sandwich ruthenium(II) and rhodium(III) thiosemicarbazone complexes

被引：52

作者：

Adams, Muneebah ^{[1
]}

de Kock, Carmen ^{[2
]}

Smith, Peter J. ^{[2
]}

Land, Kirkwood M. ^{[3
]}

Liu, Nicole ^{[3
]}

Hopper, Melissa ^{[3
]}

Hsiao, Allyson ^{[3
]}

Burgoyne, Andrew R. ^{[1
]}

Stringer, Tameryn ^{[1
]}

Meyer, Mervin ^{[4
]}

Wiesner, Lubbe ^{[2
]}

Chibale, Kelly ^{[1
,5
,6
]}

Smith, Gregory S. ^{[1
]}

机构：

[1] Univ Cape Town, Dept Chem, ZA-7701 Cape Town, South Africa

[2] Univ Cape Town, Dept Med, Div Clin Pharmacol, ZA-7925 Cape Town, South Africa

[3] Univ Pacific, Dept Biol Sci, Stockton, CA 95211 USA

[4] Univ Western Cape, Dept Biotechnol, ZA-7535 Cape Town, South Africa

[5] Univ Cape Town, Inst Infect Dis & Mol Med, ZA-7701 Rondebosch, South Africa

[6] Univ Cape Town, South African Med Res Council Drug Discovery & De, ZA-7701 Rondebosch, South Africa

来源：

DALTON TRANSACTIONS | 2015年 / 44卷 / 05期

基金：

英国医学研究理事会; 新加坡国家研究基金会;

关键词：

IN-VITRO; TRICHOMONAS-VAGINALIS; ANTIPLASMODIAL EVALUATION; ANTIMALARIAL ACTIVITY; ARENE COMPLEXES; PLASMODIUM-FALCIPARUM; ANTICANCER ACTIVITY; CHLOROQUINE ANALOG; TRYPANOSOMA-CRUZI; PROSTATE-CANCER;

D O I：

10.1039/c4dt03234a

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

A series of ferrocenyl- and aryl-functionalised organosilane thiosemicarbazone compounds was obtained via a nucleophilic substitution reaction with an amine-terminated organosilane. The thiosemicarbazone (TSC) ligands were further reacted with either a ruthenium dimer [(eta(6)-(PrC6H4Me)-Pr-i)Ru(mu-Cl)Cl](2) or a rhodium dimer [(Cp*)-Rh(mu-Cl)Cl](2) to yield a series of cationic mono- and binuclear complexes. The thiosemicarbazone ligands, as well as their metal complexes, were characterised using NMR and IR spectroscopy, and mass spectrometry. The molecular structure of the binuclear ruthenium(II) complex was determined by single-crystal X-ray diffraction analysis. The thiosemicarbazones and their complexes were evaluated for their in vitro antiplasmodial activities against the chloroquine-sensitive (NF54) and chloroquine-resistant (Dd2) Plasmodium falciparum strains, displaying activities in the low micromolar range. Selected compounds were screened for potential beta-haematin inhibition activity, and it was found that two Rh(III) complexes exhibited moderate to good inhibition. Furthermore, the compounds were screened for their antitrichomonal activities against the G3 Trichomonas vaginalis strain, revealing a higher percentage of growth inhibition for the ruthenium and rhodium complexes over their corresponding ligand.

引用

页码：2456 / 2468

页数：13

共 64 条

[1] Heterobimetallic ferrocenylthiosemicarbazone palladium(II) complexes: Synthesis, electrochemistry and antiplasmodial evaluation [J].