A5039883783- Radiopharmaceutical Chemistry and Applications
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Metal complexes synthesis and properties
- Medical Imaging and Pathology Studies
- Peptidase Inhibition and Analysis
- Medical Imaging Techniques and Applications
- Lanthanide and Transition Metal Complexes
- Orthopaedic implants and arthroplasty
- Organometallic Complex Synthesis and Catalysis
- Crystallography and molecular interactions
- Lung Cancer Treatments and Mutations
- HER2/EGFR in Cancer Research
- Orthopedic Infections and Treatments
- Metal-Organic Frameworks: Synthesis and Applications
- Chemical Synthesis and Analysis
- Radioactive element chemistry and processing
- Click Chemistry and Applications
- Monoclonal and Polyclonal Antibodies Research
- Bone health and treatments
- Cellular Mechanics and Interactions
- Amyloidosis: Diagnosis, Treatment, Outcomes
- Macrophage Migration Inhibitory Factor
- Immune Response and Inflammation
- Inorganic Chemistry and Materials
National Centre of Scientific Research "Demokritos"
2015-2024
Institute of Nuclear & Radiological Sciences and Technology, Energy & Safety
2015-2024
Institute of Biosciences & Applications
2013
National and Kapodistrian University of Athens
2005-2008
Centro Uruguayo de Imagenología Molecular
2007
Aristotle University of Thessaloniki
1983-2006
University of Missouri
2003
The synthesis of M(I)(CO)(3)(NNO) (M = Re, (99m)Tc) complexes conjugated to the antitumor agent 2-(4'-aminophenyl)benzothiazole and its 6-methyl derivative, as well their in vitro vivo biological evaluation breast cancer radiopharmaceuticals, is reported. Re displayed under fluorescence microscope clear uptake by sensitive pharmacophore cell lines MCF-7 T47D, while less normal fibroblasts was much weaker. In accordance, corresponding radioactive (99m)Tc clearly higher MDA-231 compared...
The synthesis and characterization of “2 + 1” complexes the [M(CO)3]+ (M = Re, 99mTc) core with β-diketones acetylacetone (complexes 2, 8) curcumin 5, 10 6, 11) as bidentate OO ligands, imidazole or isocyanocyclohexane monodentate ligands is reported. were synthesized by reacting [NEt4]2[Re(CO)3Br3] precursor β-diketone to generate intermediate aqua complex fac-Re(CO)3(OO)(H2O) that was isolated characterized, followed replacement labile water ligand. All characterized mass spectrometry, NMR...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTTridentate ligands containing the SNS donor atom set as a novel backbone for development of technetium brain-imaging agentsSpiros G. Mastrostamatis, Minas S. Papadopoulos, Ioannis C. Pirmettis, Evagelia Paschali, Alexandra D. Varvarigou, Chariklia I. Stassinopoulou, Cathrine P. Raptopoulou, Aris Terzis, and Efstratios ChiotellisCite this: J. Med. Chem. 1994, 37, 20, 3212–3218Publication Date (Print):September 1, 1994Publication History Published...
The synthesis and characterization of neutral mixed ligand complexes fac-[M(CO)3(P)(OO)] cis-trans-[M(CO)2(P)2(OO)] (M = Re, 99mTc), with deprotonated acetylacetone or curcumin as the OO donor bidentate ligands a phosphine (triphenylphosphine methyldiphenylphosphine) monodentate P ligand, is described. were synthesized through corresponding fac-[M(CO)3(H2O)(OO)] 99mTc) intermediate aqua complex. In presence phosphine, replacement H2O molecule complex at room temperature generates tricarbonyl...
The aim of the present study is to synthesize new mannosylated dextran derivative that can be labeled with Tc-99m for potential use in sentinel lymph node detection (SLND). compound was designed have a molecular weight 10 kDa as backbone, mannose binding receptors and S-derivatized cysteine suitable chelator labeling [(99m)Tc(H(2)O)(3)(CO)(3)](+) precursor. Reaction allyl bromide (MW 11800) yielded intermediate allyl-dextran (1) about 40% coupling. Addition resulted cysteine, DC15 (2). final...
A series of 22 mixed-ligand complexes the general formula TcOL1L2, where L1H2 are N-substituted bis(2-mercaptoethyl)amine ligands, [SN(R)S], and L2H monodentate thiols as coligand, is reported. The were prepared by ligand exchange method using Tc−gluconate precursor equimolar quantities two ligands. In all cases syn stereoisomer was formed in high yield isolated a crystalline product. four HPLC analysis demonstrated presence anti reaction mixture. Although less than 1%, one isomer, 4a,...
The synthesis and biological evaluation of new M(I)(CO)3(NNO) (M = Re, 99mTc) complexes attached to the antitumor agent 2-(4-aminophenyl)benzothiazole are reported. fluorescent rhenium complex enters MCF-7 breast cancer cells but does not enter normal HFFF-2 MRC-5 cells. analogous radioactive 99mTc produces fast blood soft tissue clearance when administered healthy mice. These promising candidates for developing radiopharmaceuticals imaging (99mTc) targeted radiotherapy (186Re, 188Re) cancer.
Two series of [99mTc](SNS/S) mixed ligand complexes each carrying the N-diethylaminoethyl or N-ethyl-substituted bis(2-mercaptoethyl)amine (SNS) are produced at tracer level using tin chloride as reductant and glucoheptonate transfer ligand. The identity is established by high-performance liquid chromatographic (HPLC) comparison with authentic rhenium samples. para substituent R on phenylthiolate coligand (S) ranges from electron-donating (−NH2) to electron-withdrawing (−NO2) groups, study...
The simultaneous action of the tridentate ligand (C(2)H(5))(2)NCH(2)CH(2)N(CH(2)CH(2)SH)(2) and monodentate coligand HSC(6)H(4)OCH(3) on a suitable ReO(3+) precursor results in mixture syn- anti-oxorhenium complexes, ReO[(C(2)H(5))(2)NCH(2)CH(2)N(CH(2)CH(2)S)(2)] [SC(6)H(4)OCH(3)], ratio 25/1. complexes are prepared by exchange reaction using ReO(eg)(2) (eg = ethylene glycol), ReOCl(3)(PPh(3))(2), or Re(V)-citrate as precursor. Both have been characterized elemental analysis, FT-IR, UV-vis,...
The reaction of fac-[NEt(4)](2)[Re(CO)(3)Br(3)] with (S)-(2-(2'-pyridyl)ethyl)cysteamine, L(1), in methanol leads to the formation cationic fac-[Re(CO)(3)(NSN)][Br] complex, 1, coordination nitrogen pyridine, sulfur thioether, and primary amine. When reacts homocysteine derivative (S)-(2-(2'-pyridyl)ethyl)-d,l-homocysteine, L(2), neutral fac-Re(CO)(3)(NSO) 2, is produced amine, oxygen carboxylate group, while pyridine ring remains uncoordinated. analogous technetium-99m complexes, 1' 2',...
In the present work, we investigated potential means to obtain neutral tricarbonyl mixed-ligand fac-[M(CO)3L1L2] complexes (M = Re, 99mTc) containing (2-hydroxyphenyl)diphenylphosphine (POH) bidentate ligand (L1H) and a series of monodentate ligands (L2). First, fac-[Re(CO)3(PO)(H2O)], 1, was synthesized by reaction POH [Et4N]2[Re(CO)3Br3] in equimolar amounts MeOH at room temperature. Interestingly, with excess this afforded fac-[Re(CO)3(PO)(POH)], 2, operating both as ligand. Owing...
The synthesis and evaluation of three novel 99mTc complexes (99mTc-1–3) their corresponding Re (Re-1–3), in which the phenyl ring 2-phenylbenzothiazole or 2-phenylbenzimidazole is replaced by cyclopentadienyl tricarbonyl [Cp99mTc(CO)3] core, are reported. Both were prepared from ferrocenyl derivatives, fully characterized elemental analysis, spectroscopic methods, X-ray crystallography. exhibit effective vitro binding to β-amyloid (Aβ) plaques fibrils, inhibit Aβ fibril formation,...
A series of neutral, lipophilic 99mTc mixed-ligand complexes the general formula 99mTcOL1L2, where L1H2 is an N-substituted bis-(2-mercaptoethyl)amine, [X-CH2CH2N(CH2CH2SH)2], [SNS], and L2H a monodentate thiol (RSH), [S], has been synthesized evaluated in rodents for potential use brain blood flow imaging. The were prepared by ligand exchange reaction using 99mTc(V)O-glucoheptonate as precursor equimolar quantities two ligands. In all cases syn isomer was formed high yield, whereas anti not...
Abstract The 2‐(4′‐aminophenyl)‐6‐methylbenzothiazole that is known to display affinity and specificity toward the amyloid plaques of Alzheimer's disease (AD) has been joined tricarbonyl [M(CO) 3 NNO] chelate (M = Re, 99 Tc, 99m Tc) through a five‐carbon linker chain generate neutral complex 1 (namely, Re‐1 for M Re; Tc‐1 Tc; with aim developing single‐photon emission computed tomography (SPECT) radiodiagnostic agent AD. was characterized by spectroscopic methods X‐ray crystallography,...
The development of a 99mTc-radiotracer for imaging β-amyloid (Aβ) plaques with single photon emission computed tomography (SPECT) is strongly anticipated to provide low cost and broadly accessible diagnostic tool Alzheimer's disease (AD). Within this framework, 2-(4'-aminophenyl)benzothiazole, known display affinity specificity Aβ plaques, has been joined the tricarbonyl fac-[M(CO)3]+ (M = Re(I), 99mTc(I)) core through cyclopentadienyl moiety yield stable, neutral, lipophilic complexes (Re-1...
A new approach to the "3 + 1" mixed ligand oxotechnetium complexes of general formula TcOL1L2, with ligands (L1H(2)) containing SNN donor set and various monodentate thiols as coligands (L2H) is reported. The L1H(2) (1-3, R(1)CH(2)CH(2)NHCH(2)C(R(2))(2)SH where R(1) = N(CH(3))(2) R(2) H in 1, pyrrolidin-1-yl 2, piperidin-1-yl CH(3) 3) act tridentate chelates TcO(3+) core, leaving open one coordination site cis oxo group. In presence a thiol using (99)Tc(V)-gluconate precursor, vacancy filled...
The synthesis and characterization of the dicarbonyl mixed ligand cis-[Re(CO)2(quin)(cisc)(PPh3)] complex, 4, where quin is deprotonated quinaldic acid, cisc cyclohexyl isocyanide, PPh3 triphenylphosphine, presented. 4 proceeds in three steps. In first, intermediate fac-[Re(CO)3(quin)(H2O)] aqua complex 2 generated from fac-[NEt4]2[Re(CO)3Br3] precursor, together with brominated products fac-[Re(CO)3(quinH)(Br)] 1a fac-[NEt4][Re(CO)3(quin)(Br)] 1b, low yield. following step, replacement by...