Synthesis and in vitro evaluation of gold(I) thiosemicarbazone complexes for antimalarial activity

被引：56

作者：

Khanye, Setshaba D. ^{[1
]}

Smith, Gregory S. ^{[1
]}

Lategan, Carmen ^{[2
]}

Smith, Peter J. ^{[2
]}

Gut, Jiri ^{[3
]}

Rosenthal, Philip J. ^{[3
]}

Chibale, Kelly ^{[1
,4
]}

机构：

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

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

[3] Univ Calif San Francisco, San Francisco Gen Hosp, Dept Med, San Francisco, CA 94143 USA

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

来源：

JOURNAL OF INORGANIC BIOCHEMISTRY | 2010年 / 104卷 / 10期

基金：

新加坡国家研究基金会;

关键词：

Falcipain-2; Gold(I) complexes; P; falciparum; Thiosemicarbazones; METAL-BASED CHEMOTHERAPY; PLASMODIUM-FALCIPARUM; CYSTEINE PROTEASE; TROPICAL DISEASES; CHLOROQUINE; DERIVATIVES; INHIBITORS; CHEMISTRY; MALARIA; SEMICARBAZONES;

D O I：

10.1016/j.jinorgbio.2010.06.005

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The reaction of thiosemicarbazones (TSCs) with [Au-I(THT)CI], THT = tetrahydrothiophene, has been investigated. The resulting gold(I) complexes have been characterized by a range of spectroscopic techniques: NMR spectroscopy. mass spectrometry, microanalysis and infrared spectroscopy. The in vitro antimalarial data for gold(I) TSC complexes suggests that coordination of gold(I) to TSCs enhanced their efficacy against the malaria parasite Plasmodium falciparum and their inhibition of the parasite cysteine protease falcipain-2. (c) 2010 Elsevier Inc. All rights reserved.

引用

页码：1079 / 1083

页数：5

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