212697-53-5Relevant academic research and scientific papers
Tetraazamacrocyclic derivatives and their metal complexes as antileishmanial leads
Hubin, Timothy J.,Walker, Ashlie N.,Davilla, Dustin J.,Carder Freeman, TaRynn N.,Epley, Brittany M.,Hasley, Travis R.,Amoyaw, Prince N.A.,Jain, Surendra,Archibald, Stephen J.,Prior, Timothy J.,Krause, Jeanette A.,Oliver, Allen G.,Tekwani, Babu L.,Khan, M. Omar F.
, p. 42 - 53 (2019/03/04)
A total of 44 bis-aryl-monocyclic polyamines, monoaryl-monocyclic polyamines and their transition metal complexes were prepared, chemically characterized, and screened in vitro against the Leishmania donovani promastigotes, axenic amastigotes and intracellular amastigotes in THP1 cells. The IC50 and/or IC90 values showed that 10 compounds were similarly active at about 2-fold less potent than known drug pentamidine against promastigotes. The most potent compound had an IC50 of 2.82 μM (compared to 2.93 μM for pentamidine). Nine compounds were 1.1–13.6-fold more potent than pentamidine against axenic amastigotes, the most potent one being about 2-fold less potent than amphotericin B. Fourteen compounds were about 2–10 fold more potent than pentamidine, the most potent one is about 2-fold less potent than amphotericin B against intracellular amastigotes in THP1 cells. The 2 most promising compounds (FeL7Cl2 and MnL7Cl2), with strong activity against both promastigotes and amastigotes and no observable toxicity against the THP1 cells are the Fe2+- and Mn2+-complexes of a dibenzyl cyclen derivative. Only 2 of the 44 compounds showed observable cytotoxicity against THP1 cells. Tetraazamacrocyclic monocyclic polyamines represent a new class of antileishmanial lead structures that warrant follow up studies.
Iron(III) Complexes with Cross-Bridged Cyclams: Synthesis and Use in Alcohol and Water Oxidation Catalysis
Annunziata, Alfonso,Esposito, Roberto,Gatto, Giordano,Cucciolito, Maria Elena,Tuzi, Angela,Macchioni, Alceo,Ruffo, Francesco
, p. 3304 - 3311 (2018/07/31)
A class of iron(III) complexes containing diversely substituted cross-bridged cyclams (1-R,R′: 1-Me,Me, 1-Me,Et, 1-Et,Et, 1-Me,Bn, 1-Bn,Bn) has been prepared and characterized. (1-R,R′) complexes catalyze the oxidation of alcohols to ketones in green cond
Challenges in chelating positron emitting copper isotopes: Tailored synthesis of unsymmetric chelators to form ultra stable complexes
Silversides, Jon D.,Smith, Rachel,Archibald, Stephen J.
experimental part, p. 6289 - 6297 (2011/08/02)
The synthesis of chelators that form high stability complexes with copper(ii) isotopes and do not suffer from transchelation in vivo has been a goal for many chemists. Such chelators will facilitate the exploitation of the 64Cu isotope (t1/2 = 12.7 h, β+ (19%); β- (39%); EC (41%)) for positron emission tomography imaging studies, which has a longer half life relative to the more commonly used 18F (t1/2 = 109.8 min) and 11C (t1/2 = 20.4 min) isotopes. One option is the CBTE2A chelator, which has been championed by Weisman, Wong and Anderson, and, more recently, alternate bifunctional chelator (BFC) versions have been synthesised. Improved synthetic methods are required for unsymmetric derivatisation of these chelators to allow more selective biomolecule attachment. This work investigates synthetic routes to form new unsymmetric chelating ligands via stepwise reaction of the bisaminal precursor, determines their X-ray structures and demonstrates cold copper(ii) isotope complex formation.
